Loading...
Header Logo
Keywords
Last Name
Institution

Dr Ian Hugh Gilbert

Title[no position]
Institution[no institution name]
Address[no address]
vCardDownload vCard

    Collapse Bibliographic 
    Collapse selected publications
    Publications listed below are automatically derived from MEDLINE/PubMed and other sources, which might result in incorrect or missing publications. Faculty can login to make corrections and additions.
    List All   |   Timeline
    1. Ray PC, Kiczun M, Huggett M, Lim A, Prati F, Gilbert IH, Wyatt PG. Fragment library design, synthesis and expansion: nurturing a synthesis and training platform. Drug Discov Today. 2017 Jan; 22(1):43-56. PMID: 27793744.
      View in: PubMed
    2. Cleghorn LA, Albrecht S, Stojanovski L, Simeons FR, Norval S, Kime R, Collie IT, De Rycker M, Campbell L, Hallyburton I, Frearson JA, Wyatt PG, Read KD, Gilbert IH. Discovery of Indoline-2-carboxamide Derivatives as a New Class of Brain-Penetrant Inhibitors of Trypanosoma brucei. J Med Chem. 2015 Oct 08; 58(19):7695-706. PMID: 26418485; PMCID: PMC4601051.
    3. Spinks D, Smith V, Thompson S, Robinson DA, Luksch T, Smith A, Torrie LS, McElroy S, Stojanovski L, Norval S, Collie IT, Hallyburton I, Rao B, Brand S, Brenk R, Frearson JA, Read KD, Wyatt PG, Gilbert IH. Development of Small-Molecule Trypanosoma brucei N-Myristoyltransferase Inhibitors: Discovery and Optimisation of a Novel Binding Mode. ChemMedChem. 2015 Nov; 10(11):1821-36. PMID: 26395087; PMCID: PMC4648043.
    4. Woodland A, Thompson S, Cleghorn LA, Norcross N, De Rycker M, Grimaldi R, Hallyburton I, Rao B, Norval S, Stojanovski L, Brun R, Kaiser M, Frearson JA, Gray DW, Wyatt PG, Read KD, Gilbert IH. Discovery of Inhibitors of Trypanosoma brucei by Phenotypic Screening of a Focused Protein Kinase Library. ChemMedChem. 2015 Nov; 10(11):1809-20. PMID: 26381210; PMCID: PMC4648050.
    5. Mital A, Murugesan D, Kaiser M, Yeates C, Gilbert IH. Discovery and optimisation studies of antimalarial phenotypic hits. Eur J Med Chem. 2015 Oct 20; 103:530-8. PMID: 26408453; PMCID: PMC4607724.
    6. Baragaña B, Hallyburton I, Lee MC, Norcross NR, Grimaldi R, Otto TD, Proto WR, Blagborough AM, Meister S, Wirjanata G, Ruecker A, Upton LM, Abraham TS, Almeida MJ, Pradhan A, Porzelle A. A novel multiple-stage antimalarial agent that inhibits protein synthesis. Nature. 2015 06 18; 522(7556):315-20. PMID: 26085270; PMCID: PMC4700930.
    7. Guidi A, Mansour NR, Paveley RA, Carruthers IM, Besnard J, Hopkins AL, Gilbert IH, Bickle QD. Application of RNAi to Genomic Drug Target Validation in Schistosomes. PLoS Negl Trop Dis. 2015 May; 9(5):e0003801. PMID: 25992548; PMCID: PMC4438872.
    8. Fang W, Robinson DA, Raimi OG, Blair DE, Harrison JR, Lockhart DE, Torrie LS, Ruda GF, Wyatt PG, Gilbert IH, van Aalten DM. N-myristoyltransferase is a cell wall target in Aspergillus fumigatus. ACS Chem Biol. 2015 Jun 19; 10(6):1425-34. PMID: 25706802; PMCID: PMC4477619.
    9. Henderson CJ, McLaughlin LA, Osuna-Cabello M, Taylor M, Gilbert I, McLaren AW, Wolf CR. Application of a novel regulatable Cre recombinase system to define the role of liver and gut metabolism in drug oral bioavailability. Biochem J. 2015 Feb 01; 465(3):479-88. PMID: 25377919.
      View in: PubMed
    10. Brand S, Norcross NR, Thompson S, Harrison JR, Smith VC, Robinson DA, Torrie LS, McElroy SP, Hallyburton I, Norval S, Scullion P, Stojanovski L, Simeons FR, van Aalten D, Frearson JA, Brenk R, Fairlamb AH, Ferguson MA, Wyatt PG, Gilbert IH, Read KD. Lead optimization of a pyrazole sulfonamide series of Trypanosoma brucei N-myristoyltransferase inhibitors: identification and evaluation of CNS penetrant compounds as potential treatments for stage 2 human African trypanosomiasis. J Med Chem. 2014 Dec 11; 57(23):9855-69. PMID: 25412409; PMCID: PMC4269550.
    11. Giordani F, Buschini A, Baliani A, Kaiser M, Brun R, Barrett MP, Pellacani C, Poli P, Gilbert IH. Characterization of a melamino nitroheterocycle as a potential lead for the treatment of human african trypanosomiasis. Antimicrob Agents Chemother. 2014 Oct; 58(10):5747-57. PMID: 25022590; PMCID: PMC4187918.
    12. Capes AS, Crossman A, Urbaniak MD, Gilbert SH, Ferguson MA, Gilbert IH. Probing the substrate specificity of Trypanosoma brucei GlcNAc-PI de-N-acetylase with synthetic substrate analogues. Org Biomol Chem. 2014 Mar 28; 12(12):1919-34. PMID: 24519084; PMCID: PMC4326964.
    13. Urbaniak MD, Capes AS, Crossman A, O'Neill S, Thompson S, Gilbert IH, Ferguson MA. Fragment screening reveals salicylic hydroxamic acid as an inhibitor of Trypanosoma brucei GPI GlcNAc-PI de-N-acetylase. Carbohydr Res. 2014 Mar 31; 387:54-8. PMID: 24589444; PMCID: PMC3991331.
    14. Kerkhoven EJ, Achcar F, Alibu VP, Burchmore RJ, Gilbert IH, Trybilo M, Driessen NN, Gilbert D, Breitling R, Bakker BM, Barrett MP. Handling uncertainty in dynamic models: the pentose phosphate pathway in Trypanosoma brucei. PLoS Comput Biol. 2013; 9(12):e1003371. PMID: 24339766; PMCID: PMC3854711.
    15. Pizarro JC, Hills T, Senisterra G, Wernimont AK, Mackenzie C, Norcross NR, Ferguson MA, Wyatt PG, Gilbert IH, Hui R. Exploring the Trypanosoma brucei Hsp83 potential as a target for structure guided drug design. PLoS Negl Trop Dis. 2013; 7(10):e2492. PMID: 24147171; PMCID: PMC3798429.
    16. Gilbert IH. Drug discovery for neglected diseases: molecular target-based and phenotypic approaches. J Med Chem. 2013 Oct 24; 56(20):7719-26. PMID: 24015767; PMCID: PMC3954685.
    17. Gilbert IH. Target-based drug discovery for human African trypanosomiasis: selection of molecular target and chemical matter. Parasitology. 2014 Jan; 141(1):28-36. PMID: 23931634; PMCID: PMC3884840.
    18. Murugesan D, Kaiser M, White KL, Norval S, Riley J, Wyatt PG, Charman SA, Read KD, Yeates C, Gilbert IH. Structure-activity relationship studies of pyrrolone antimalarial agents. ChemMedChem. 2013 Sep; 8(9):1537-44. PMID: 23918316; PMCID: PMC3963473.
    19. Morley AD, Pugliese A, Birchall K, Bower J, Brennan P, Brown N, Chapman T, Drysdale M, Gilbert IH, Hoelder S, Jordan A, Ley SV, Merritt A, Miller D, Swarbrick ME, Wyatt PG. Fragment-based hit identification: thinking in 3D. Drug Discov Today. 2013 Dec; 18(23-24):1221-7. PMID: 23906694.
      View in: PubMed
    20. Hampton SE, Schipani A, Bosch-Navarrete C, Recio E, Kaiser M, Kahnberg P, González-Pacanowska D, Johansson NG, Gilbert IH. Investigation of acyclic uridine amide and 5'-amido nucleoside analogues as potential inhibitors of the Plasmodium falciparum dUTPase. Bioorg Med Chem. 2013 Sep 15; 21(18):5876-85. PMID: 23916149; PMCID: PMC3776224.
    21. Woodland A, Grimaldi R, Luksch T, Cleghorn LA, Ojo KK, Van Voorhis WC, Brenk R, Frearson JA, Gilbert IH, Wyatt PG. From on-target to off-target activity: identification and optimisation of Trypanosoma brucei GSK3 inhibitors and their characterisation as anti-Trypanosoma brucei drug discovery lead molecules. ChemMedChem. 2013 Jul; 8(7):1127-37. PMID: 23776181; PMCID: PMC3728731.
    22. De Rycker M, Hallyburton I, Thomas J, Campbell L, Wyllie S, Joshi D, Cameron S, Gilbert IH, Wyatt PG, Frearson JA, Fairlamb AH, Gray DW. Comparison of a high-throughput high-content intracellular Leishmania donovani assay with an axenic amastigote assay. Antimicrob Agents Chemother. 2013 Jul; 57(7):2913-22. PMID: 23571538; PMCID: PMC3697379.
    23. Murugesan D, Mital A, Kaiser M, Shackleford DM, Morizzi J, Katneni K, Campbell M, Hudson A, Charman SA, Yeates C, Gilbert IH. Discovery and structure-activity relationships of pyrrolone antimalarials. J Med Chem. 2013 Apr 11; 56(7):2975-90. PMID: 23517371; PMCID: PMC3624797.
    24. Cui H, Carrero-Lérida J, Silva AP, Whittingham JL, Brannigan JA, Ruiz-Pérez LM, Read KD, Wilson KS, González-Pacanowska D, Gilbert IH. Synthesis and evaluation of a-thymidine analogues as novel antimalarials. J Med Chem. 2012 Dec 27; 55(24):10948-57. PMID: 23240776; PMCID: PMC3530961.
    25. Besnard J, Ruda GF, Setola V, Abecassis K, Rodriguiz RM, Huang XP, Norval S, Sassano MF, Shin AI, Webster LA, Simeons FR, Stojanovski L, Prat A, Seidah NG, Constam DB, Bickerton GR, Read KD, Wetsel WC, Gilbert IH, Roth BL, Hopkins AL. Automated design of ligands to polypharmacological profiles. Nature. 2012 Dec 13; 492(7428):215-20. PMID: 23235874; PMCID: PMC3653568.
    26. Paveley RA, Mansour NR, Hallyburton I, Bleicher LS, Benn AE, Mikic I, Guidi A, Gilbert IH, Hopkins AL, Bickle QD. Whole organism high-content screening by label-free, image-based Bayesian classification for parasitic diseases. PLoS Negl Trop Dis. 2012; 6(7):e1762. PMID: 22860151; PMCID: PMC3409125.
    27. Capes A, Patterson S, Wyllie S, Hallyburton I, Collie IT, McCarroll AJ, Stevens MF, Frearson JA, Wyatt PG, Fairlamb AH, Gilbert IH. Quinol derivatives as potential trypanocidal agents. Bioorg Med Chem. 2012 Feb 15; 20(4):1607-15. PMID: 22264753; PMCID: PMC3281193.
    28. Spinks D, Torrie LS, Thompson S, Harrison JR, Frearson JA, Read KD, Fairlamb AH, Wyatt PG, Gilbert IH. Design, synthesis and biological evaluation of Trypanosoma brucei trypanothione synthetase inhibitors. ChemMedChem. 2012 Jan 02; 7(1):95-106. PMID: 22162199; PMCID: PMC3320663.
    29. Brand S, Cleghorn LA, McElroy SP, Robinson DA, Smith VC, Hallyburton I, Harrison JR, Norcross NR, Spinks D, Bayliss T, Norval S, Stojanovski L, Torrie LS, Frearson JA, Brenk R, Fairlamb AH, Ferguson MA, Read KD, Wyatt PG, Gilbert IH. Discovery of a novel class of orally active trypanocidal N-myristoyltransferase inhibitors. J Med Chem. 2012 Jan 12; 55(1):140-52. PMID: 22148754; PMCID: PMC3256935.
    30. Hampton SE, Baragaña B, Schipani A, Bosch-Navarrete C, Musso-Buendía JA, Recio E, Kaiser M, Whittingham JL, Roberts SM, Shevtsov M, Brannigan JA, Kahnberg P, Brun R, Wilson KS, González-Pacanowska D, Johansson NG, Gilbert IH. Design, synthesis, and evaluation of 5'-diphenyl nucleoside analogues as inhibitors of the Plasmodium falciparum dUTPase. ChemMedChem. 2011 Oct 04; 6(10):1816-31. PMID: 22049550.
      View in: PubMed
    31. Cleghorn LA, Woodland A, Collie IT, Torrie LS, Norcross N, Luksch T, Mpamhanga C, Walker RG, Mottram JC, Brenk R, Frearson JA, Gilbert IH, Wyatt PG. Identification of inhibitors of the Leishmania cdc2-related protein kinase CRK3. ChemMedChem. 2011 Dec 09; 6(12):2214-24. PMID: 21913331; PMCID: PMC3272345.
    32. Patterson S, Alphey MS, Jones DC, Shanks EJ, Street IP, Frearson JA, Wyatt PG, Gilbert IH, Fairlamb AH. Dihydroquinazolines as a novel class of Trypanosoma brucei trypanothione reductase inhibitors: discovery, synthesis, and characterization of their binding mode by protein crystallography. J Med Chem. 2011 Oct 13; 54(19):6514-30. PMID: 21851087; PMCID: PMC3188286.
    33. Smith VC, Cleghorn LA, Woodland A, Spinks D, Hallyburton I, Collie IT, Mok NY, Norval S, Brenk R, Fairlamb AH, Frearson JA, Read KD, Gilbert IH, Wyatt PG. Optimisation of the anti-Trypanosoma brucei activity of the opioid agonist U50488. ChemMedChem. 2011 Oct 04; 6(10):1832-40. PMID: 21834094; PMCID: PMC3229842.
    34. Recio E, Musso-Buendía A, Vidal AE, Ruda GF, Kasinathan G, Nguyen C, Ruiz-Pérez LM, Gilbert IH, González-Pacanowska D. Site-directed mutagenesis provides insights into the selective binding of trityl derivatives to Plasmodium falciparum dUTPase. Eur J Med Chem. 2011 Aug; 46(8):3309-14. PMID: 21600680.
      View in: PubMed
    35. Baragaña B, McCarthy O, Sánchez P, Bosch-Navarrete C, Kaiser M, Brun R, Whittingham JL, Roberts SM, Zhou XX, Wilson KS, Johansson NG, González-Pacanowska D, Gilbert IH. ß-Branched acyclic nucleoside analogues as inhibitors of Plasmodium falciparum dUTPase. Bioorg Med Chem. 2011 Apr 01; 19(7):2378-91. PMID: 21411327.
      View in: PubMed
    36. Ishida K, Fernandes Rodrigues JC, Cammerer S, Urbina JA, Gilbert I, de Souza W, Rozental S. Synthetic arylquinuclidine derivatives exhibit antifungal activity against Candida albicans, Candida tropicalis and Candida parapsilopsis. Ann Clin Microbiol Antimicrob. 2011 Jan 21; 10:3. PMID: 21255433; PMCID: PMC3036746.
    37. Ruda GF, Nguyen C, Ziemkowski P, Felczak K, Kasinathan G, Musso-Buendia A, Sund C, Zhou XX, Kaiser M, Ruiz-Pérez LM, Brun R, Kulikowski T, Johansson NG, González-Pacanowska D, Gilbert IH. Modified 5'-trityl nucleosides as inhibitors of Plasmodium falciparum dUTPase. ChemMedChem. 2011 Feb 07; 6(2):309-20. PMID: 21246738.
      View in: PubMed
    38. Gilbert IH, Leroy D, Frearson JA. Finding new hits in neglected disease projects: target or phenotypic based screening? Curr Top Med Chem. 2011; 11(10):1284-91. PMID: 21401505.
      View in: PubMed
    39. Wyatt PG, Gilbert IH, Read KD, Fairlamb AH. Target validation: linking target and chemical properties to desired product profile. Curr Top Med Chem. 2011; 11(10):1275-83. PMID: 21401506; PMCID: PMC3182078.
    40. Spinks D, Ong HB, Mpamhanga CP, Shanks EJ, Robinson DA, Collie IT, Read KD, Frearson JA, Wyatt PG, Brenk R, Fairlamb AH, Gilbert IH. Design, synthesis and biological evaluation of novel inhibitors of Trypanosoma brucei pteridine reductase 1. ChemMedChem. 2011 Feb 07; 6(2):302-8. PMID: 21275054; PMCID: PMC3047710.
    41. Martins-Duarte ES, Lemgruber L, Lorente SO, Gros L, Magaraci F, Gilbert IH, de Souza W, Vommaro RC. Evaluation of three novel azasterols against Toxoplasma gondii. Vet Parasitol. 2011 Apr 19; 177(1-2):157-61. PMID: 21176865.
      View in: PubMed
    42. Schüttelkopf AW, Gros L, Blair DE, Frearson JA, van Aalten DM, Gilbert IH. Acetazolamide-based fungal chitinase inhibitors. Bioorg Med Chem. 2010 Dec 01; 18(23):8334-40. PMID: 21044846; PMCID: PMC2997425.
    43. Ruda GF, Wong PE, Alibu VP, Norval S, Read KD, Barrett MP, Gilbert IH. Aryl phosphoramidates of 5-phospho erythronohydroxamic acid, a new class of potent trypanocidal compounds. J Med Chem. 2010 Aug 26; 53(16):6071-8. PMID: 20666371; PMCID: PMC2923871.
    44. Cui H, Ruda GF, Carrero-Lérida J, Ruiz-Pérez LM, Gilbert IH, González-Pacanowska D. Exploring new inhibitors of Plasmodium falciparum purine nucleoside phosphorylase. Eur J Med Chem. 2010 Nov; 45(11):5140-9. PMID: 20817362.
      View in: PubMed
    45. Gigante F, Kaiser M, Brun R, Gilbert IH. Design and preparation of sterol mimetics as potential antiparasitics. Bioorg Med Chem. 2010 Oct 15; 18(20):7291-301. PMID: 20846867.
      View in: PubMed
    46. Cui H, Ruiz-Pérez LM, González-Pacanowska D, Gilbert IH. Potential application of thymidylate kinase in nucleoside analogue activation in Plasmodium falciparum. Bioorg Med Chem. 2010 Oct 15; 18(20):7302-9. PMID: 20833052.
      View in: PubMed
    47. Klee N, Wong PE, Baragaña B, Mazouni FE, Phillips MA, Barrett MP, Gilbert IH. Selective delivery of 2-hydroxy APA to Trypanosoma brucei using the melamine motif. Bioorg Med Chem Lett. 2010 Aug 01; 20(15):4364-6. PMID: 20615694; PMCID: PMC2935964.
    48. Ruda GF, Campbell G, Alibu VP, Barrett MP, Brenk R, Gilbert IH. Virtual fragment screening for novel inhibitors of 6-phosphogluconate dehydrogenase. Bioorg Med Chem. 2010 Jul 15; 18(14):5056-62. PMID: 20598892; PMCID: PMC2939770.
    49. Whittingham JL, Carrero-Lerida J, Brannigan JA, Ruiz-Perez LM, Silva AP, Fogg MJ, Wilkinson AJ, Gilbert IH, Wilson KS, González-Pacanowska D. Structural basis for the efficient phosphorylation of AZT-MP (3'-azido-3'-deoxythymidine monophosphate) and dGMP by Plasmodium falciparum type I thymidylate kinase. Biochem J. 2010 May 27; 428(3):499-509. PMID: 20353400.
      View in: PubMed
    50. Frearson JA, Brand S, McElroy SP, Cleghorn LA, Smid O, Stojanovski L, Price HP, Guther ML, Torrie LS, Robinson DA, Hallyburton I, Mpamhanga CP, Brannigan JA, Wilkinson AJ, Hodgkinson M, Hui R, Qiu W, Raimi OG, van Aalten DM, Brenk R, Gilbert IH, Read KD, Fairlamb AH, Ferguson MA, Smith DF, Wyatt PG. N-myristoyltransferase inhibitors as new leads to treat sleeping sickness. Nature. 2010 Apr 01; 464(7289):728-32. PMID: 20360736; PMCID: PMC2917743.
    51. Nicoletti S, Seifert K, Gilbert IH. Water-soluble polymer-drug conjugates for combination chemotherapy against visceral leishmaniasis. Bioorg Med Chem. 2010 Apr 01; 18(7):2559-65. PMID: 20338769; PMCID: PMC2862900.
    52. Spinks D, Shanks EJ, Cleghorn LA, McElroy S, Jones D, James D, Fairlamb AH, Frearson JA, Wyatt PG, Gilbert IH. Investigation of trypanothione reductase as a drug target in Trypanosoma brucei. ChemMedChem. 2009 Dec; 4(12):2060-9. PMID: 19924760; PMCID: PMC2855869.
    53. Torrie LS, Wyllie S, Spinks D, Oza SL, Thompson S, Harrison JR, Gilbert IH, Wyatt PG, Fairlamb AH, Frearson JA. Chemical validation of trypanothione synthetase: a potential drug target for human trypanosomiasis. J Biol Chem. 2009 Dec 25; 284(52):36137-45. PMID: 19828449; PMCID: PMC2794729.
    54. Martins-Duarte ES, Jones SM, Gilbert IH, Atella GC, de Souza W, Vommaro RC. Thiolactomycin analogues as potential anti-Toxoplasma gondii agents. Parasitol Int. 2009 Dec; 58(4):411-5. PMID: 19698800.
      View in: PubMed
    55. Richardson JL, Nett IR, Jones DC, Abdille MH, Gilbert IH, Fairlamb AH. Improved tricyclic inhibitors of trypanothione reductase by screening and chemical synthesis. ChemMedChem. 2009 Aug; 4(8):1333-40. PMID: 19557801; PMCID: PMC2929371.
    56. Patterson S, Jones DC, Shanks EJ, Frearson JA, Gilbert IH, Wyatt PG, Fairlamb AH. Synthesis and evaluation of 1-(1-(Benzo[b]thiophen-2-yl)cyclohexyl)piperidine (BTCP) analogues as inhibitors of trypanothione reductase. ChemMedChem. 2009 Aug; 4(8):1341-53. PMID: 19557802; PMCID: PMC2929374.
    57. Mpamhanga CP, Spinks D, Tulloch LB, Shanks EJ, Robinson DA, Collie IT, Fairlamb AH, Wyatt PG, Frearson JA, Hunter WN, Gilbert IH, Brenk R. One scaffold, three binding modes: novel and selective pteridine reductase 1 inhibitors derived from fragment hits discovered by virtual screening. J Med Chem. 2009 Jul 23; 52(14):4454-65. PMID: 19527033; PMCID: PMC2966039.
    58. Gigante F, Kaiser M, Brun R, Gilbert IH. SAR studies on azasterols as potential anti-trypanosomal and anti-leishmanial agents. Bioorg Med Chem. 2009 Aug 15; 17(16):5950-61. PMID: 19620005.
      View in: PubMed
    59. Musso-Buendía JA, Vidal AE, Kasinthan G, Nguyen C, Carrero-Lérida J, Ruiz-Pérez LM, Wilson K, Johansson NG, Gilbert IH, González-Pacanowska D. Kinetic properties and inhibition of the dimeric dUTPase-dUDPase from Campylobacter jejuni. J Enzyme Inhib Med Chem. 2009 Feb; 24(1):111-6. PMID: 18608754.
      View in: PubMed
    60. Chollet C, Baliani A, Wong PE, Barrett MP, Gilbert IH. Targeted delivery of compounds to Trypanosoma brucei using the melamine motif. Bioorg Med Chem. 2009 Mar 15; 17(6):2512-23. PMID: 19250832.
      View in: PubMed
    61. Baliani A, Peal V, Gros L, Brun R, Kaiser M, Barrett MP, Gilbert IH. Novel functionalized melamine-based nitroheterocycles: synthesis and activity against trypanosomatid parasites. Org Biomol Chem. 2009 Mar 21; 7(6):1154-66. PMID: 19262935.
      View in: PubMed
    62. Nicoletti S, Seifert K, Gilbert IH. N-(2-hydroxypropyl)methacrylamide-amphotericin B (HPMA-AmB) copolymer conjugates as antileishmanial agents. Int J Antimicrob Agents. 2009 May; 33(5):441-8. PMID: 19097763; PMCID: PMC2669511.
    63. McCarthy O, Musso-Buendia A, Kaiser M, Brun R, Ruiz-Perez LM, Johansson NG, Pacanowska DG, Gilbert IH. Design, synthesis and evaluation of novel uracil acetamide derivatives as potential inhibitors of Plasmodium falciparum dUTP nucleotidohydrolase. Eur J Med Chem. 2009 Feb; 44(2):678-88. PMID: 18619713.
      View in: PubMed
    64. Brenk R, Schipani A, James D, Krasowski A, Gilbert IH, Frearson J, Wyatt PG. Lessons learnt from assembling screening libraries for drug discovery for neglected diseases. ChemMedChem. 2008 Mar; 3(3):435-44. PMID: 18064617; PMCID: PMC2628535.
    65. Sellarajah S, Boussard C, Lekishvili T, Brown DR, Gilbert IH. Synthesis and testing of peptides for anti-prion activity. Eur J Med Chem. 2008 Nov; 43(11):2418-27. PMID: 18355947.
      View in: PubMed
    66. Frearson JA, Wyatt PG, Gilbert IH, Fairlamb AH. Target assessment for antiparasitic drug discovery. Trends Parasitol. 2007 Dec; 23(12):589-95. PMID: 17962072; PMCID: PMC2979298.
    67. Maia C, Attias M, Urbina J, Gilbert I, Magaraci F, de Souza W. Azasterols impair Giardia lamblia proliferation and induces encystation. Biochem Biophys Res Commun. 2007 Nov 16; 363(2):310-6. PMID: 17870055.
      View in: PubMed
    68. Cammerer SB, Jimenez C, Jones S, Gros L, Lorente SO, Rodrigues C, Rodrigues JC, Caldera A, Ruiz Perez LM, da Souza W, Kaiser M, Brun R, Urbina JA, Gonzalez Pacanowska D, Gilbert IH. Quinuclidine derivatives as potential antiparasitics. Antimicrob Agents Chemother. 2007 Nov; 51(11):4049-61. PMID: 17709461; PMCID: PMC2151445.
    69. Ruda GF, Alibu VP, Mitsos C, Bidet O, Kaiser M, Brun R, Barrett MP, Gilbert IH. Synthesis and biological evaluation of phosphate prodrugs of 4-phospho-D-erythronohydroxamic acid, an inhibitor of 6-phosphogluconate dehydrogenase. ChemMedChem. 2007 Aug; 2(8):1169-80. PMID: 17615587; PMCID: PMC2248282.
    70. Webb S, Lekishvili T, Loeschner C, Sellarajah S, Prelli F, Wisniewski T, Gilbert IH, Brown DR. Mechanistic insights into the cure of prion disease by novel antiprion compounds. J Virol. 2007 Oct; 81(19):10729-41. PMID: 17652397; PMCID: PMC2045489.
    71. Granthon AC, Braga MV, Rodrigues JC, Cammerer S, Lorente SO, Gilbert IH, Urbina JA, de Souza W. Alterations on the growth and ultrastructure of Leishmania chagasi induced by squalene synthase inhibitors. Vet Parasitol. 2007 May 15; 146(1-2):25-34. PMID: 17367936.
      View in: PubMed
    72. Sealey-Cardona M, Cammerer S, Jones S, Ruiz-Pérez LM, Brun R, Gilbert IH, Urbina JA, González-Pacanowska D. Kinetic characterization of squalene synthase from Trypanosoma cruzi: selective inhibition by quinuclidine derivatives. Antimicrob Agents Chemother. 2007 Jun; 51(6):2123-9. PMID: 17371809; PMCID: PMC1891404.
    73. Sundaramoorthy R, Iulek J, Barrett MP, Bidet O, Ruda GF, Gilbert IH, Hunter WN. Crystal structures of a bacterial 6-phosphogluconate dehydrogenase reveal aspects of specificity, mechanism and mode of inhibition by analogues of high-energy reaction intermediates. FEBS J. 2007 Jan; 274(1):275-86. PMID: 17222187.
      View in: PubMed
    74. Gros L, Lorente SO, Jimenez CJ, Yardley V, Rattray L, Wharton H, Little S, Croft SL, Ruiz-Perez LM, Gonzalez-Pacanowska D, Gilbert IH. Evaluation of azasterols as anti-parasitics. J Med Chem. 2006 Oct 05; 49(20):6094-103. PMID: 17004723.
      View in: PubMed
    75. Gros L, Castillo-Acosta VM, Jiménez Jiménez C, Sealey-Cardona M, Vargas S, Manuel Estévez A, Yardley V, Rattray L, Croft SL, Ruiz-Perez LM, Urbina JA, Gilbert IH, González-Pacanowska D. New azasterols against Trypanosoma brucei: role of 24-sterol methyltransferase in inhibitor action. Antimicrob Agents Chemother. 2006 Aug; 50(8):2595-601. PMID: 16870747; PMCID: PMC1538673.
    76. Nguyen C, Ruda GF, Schipani A, Kasinathan G, Leal I, Musso-Buendia A, Kaiser M, Brun R, Ruiz-Pérez LM, Sahlberg BL, Johansson NG, Gonzalez-Pacanowska D, Gilbert IH. Acyclic nucleoside analogues as inhibitors of Plasmodium falciparum dUTPase. J Med Chem. 2006 Jul 13; 49(14):4183-95. PMID: 16821778.
      View in: PubMed
    77. Mc Carthy OK, Schipani A, Buendía AM, Ruiz-Perez LM, Kaiser M, Brun R, Pacanowska DG, Gilbert IH. Design, synthesis and evaluation of novel uracil amino acid conjugates for the inhibition of Trypanosoma cruzi dUTPase. Bioorg Med Chem Lett. 2006 Jul 15; 16(14):3809-12. PMID: 16677813.
      View in: PubMed
    78. Barrett MP, Gilbert IH. Targeting of toxic compounds to the trypanosome's interior. Adv Parasitol. 2006; 63:125-83. PMID: 17134653.
      View in: PubMed
    79. Braga MV, Magaraci F, Lorente SO, Gilbert I, de Souza W. Effects of inhibitors of Delta24(25)-sterol methyl transferase on the ultrastructure of epimastigotes of Trypanosoma cruzi. Microsc Microanal. 2005 Dec; 11(6):506-15. PMID: 17481329.
      View in: PubMed
    80. Stewart ML, Boussard C, Brun R, Gilbert IH, Barrett MP. Interaction of monobenzamidine-linked trypanocides with the Trypanosoma brucei P2 aminopurine transporter. Antimicrob Agents Chemother. 2005 Dec; 49(12):5169-71. PMID: 16304196; PMCID: PMC1315980.
    81. Nguyen C, Kasinathan G, Leal-Cortijo I, Musso-Buendia A, Kaiser M, Brun R, Ruiz-Pérez LM, Johansson NG, González-Pacanowska D, Gilbert IH. Deoxyuridine triphosphate nucleotidohydrolase as a potential antiparasitic drug target. J Med Chem. 2005 Sep 22; 48(19):5942-54. PMID: 16161998.
      View in: PubMed
    82. Jones SM, Urch JE, Kaiser M, Brun R, Harwood JL, Berry C, Gilbert IH. Analogues of thiolactomycin as potential antimalarial agents. J Med Chem. 2005 Sep 22; 48(19):5932-41. PMID: 16161997.
      View in: PubMed
    83. Lorente SO, Jimenez CJ, Gros L, Yardley V, de Luca-Fradley K, Croft SL, A Urbina J, Ruiz-Perez LM, Pacanowska DG, Gilbert IH. Preparation of transition-state analogues of sterol 24-methyl transferase as potential anti-parasitics. Bioorg Med Chem. 2005 Sep 15; 13(18):5435-53. PMID: 16046134.
      View in: PubMed
    84. Baliani A, Bueno GJ, Stewart ML, Yardley V, Brun R, Barrett MP, Gilbert IH. Design and synthesis of a series of melamine-based nitroheterocycles with activity against Trypanosomatid parasites. J Med Chem. 2005 Aug 25; 48(17):5570-9. PMID: 16107157.
      View in: PubMed
    85. Orenes Lorente S, Gómez R, Jiménez C, Cammerer S, Yardley V, de Luca-Fradley K, Croft SL, Ruiz Perez LM, Urbina J, Gonzalez Pacanowska D, Gilbert IH. Biphenylquinuclidines as inhibitors of squalene synthase and growth of parasitic protozoa. Bioorg Med Chem. 2005 May 16; 13(10):3519-29. PMID: 15848765.
      View in: PubMed
    86. Khabnadideh S, Pez D, Musso A, Brun R, Pérez LM, González-Pacanowska D, Gilbert IH. Design, synthesis and evaluation of 2,4-diaminoquinazolines as inhibitors of trypanosomal and leishmanial dihydrofolate reductase. Bioorg Med Chem. 2005 Apr 01; 13(7):2637-49. PMID: 15755663.
      View in: PubMed
    87. Whittingham JL, Leal I, Nguyen C, Kasinathan G, Bell E, Jones AF, Berry C, Benito A, Turkenburg JP, Dodson EJ, Ruiz Perez LM, Wilkinson AJ, Johansson NG, Brun R, Gilbert IH, Gonzalez Pacanowska D, Wilson KS. dUTPase as a platform for antimalarial drug design: structural basis for the selectivity of a class of nucleoside inhibitors. Structure. 2005 Feb; 13(2):329-38. PMID: 15698576.
      View in: PubMed
    88. Sellarajah S, Lekishvili T, Bowring C, Thompsett AR, Rudyk H, Birkett CR, Brown DR, Gilbert IH. Synthesis of analogues of Congo red and evaluation of their anti-prion activity. J Med Chem. 2004 Oct 21; 47(22):5515-34. PMID: 15481988.
      View in: PubMed
    89. Hanau S, Rinaldi E, Dallocchio F, Gilbert IH, Dardonville C, Adams MJ, Gover S, Barrett MP. 6-phosphogluconate dehydrogenase: a target for drugs in African trypanosomes. Curr Med Chem. 2004 Oct; 11(19):2639-50. PMID: 15544466.
      View in: PubMed
    90. Lorente SO, Rodrigues JC, Jiménez Jiménez C, Joyce-Menekse M, Rodrigues C, Croft SL, Yardley V, de Luca-Fradley K, Ruiz-Pérez LM, Urbina J, de Souza W, González Pacanowska D, Gilbert IH. Novel azasterols as potential agents for treatment of leishmaniasis and trypanosomiasis. Antimicrob Agents Chemother. 2004 Aug; 48(8):2937-50. PMID: 15273104; PMCID: PMC478520.
    91. Dardonville C, Rinaldi E, Barrett MP, Brun R, Gilbert IH, Hanau S. Selective inhibition of Trypanosoma brucei 6-phosphogluconate dehydrogenase by high-energy intermediate and transition-state analogues. J Med Chem. 2004 Jun 17; 47(13):3427-37. PMID: 15189039.
      View in: PubMed
    92. Boussard C, Klimkait T, Mahmood N, Pritchard M, Gilbert IH. Design, synthesis and evaluation of potential inhibitors of HIV gp120-CD4 interactions. Bioorg Med Chem Lett. 2004 May 17; 14(10):2673-6. PMID: 15109676.
      View in: PubMed
    93. Stewart ML, Bueno GJ, Baliani A, Klenke B, Brun R, Brock JM, Gilbert IH, Barrett MP. Trypanocidal activity of melamine-based nitroheterocycles. Antimicrob Agents Chemother. 2004 May; 48(5):1733-8. PMID: 15105128; PMCID: PMC400563.
    94. Jones SM, Urch JE, Brun R, Harwood JL, Berry C, Gilbert IH. Analogues of thiolactomycin as potential anti-malarial and anti-trypanosomal agents. Bioorg Med Chem. 2004 Feb 15; 12(4):683-92. PMID: 14759729.
      View in: PubMed
    95. Pez D, Leal I, Zuccotto F, Boussard C, Brun R, Croft SL, Yardley V, Ruiz Perez LM, Gonzalez Pacanowska D, Gilbert IH. 2,4-Diaminopyrimidines as inhibitors of Leishmanial and Trypanosomal dihydrofolate reductase. Bioorg Med Chem. 2003 Nov 03; 11(22):4693-711. PMID: 14556785.
      View in: PubMed
    96. Magaraci F, Jimenez CJ, Rodrigues C, Rodrigues JC, Braga MV, Yardley V, de Luca-Fradley K, Croft SL, de Souza W, Ruiz-Perez LM, Urbina J, Gonzalez Pacanowska D, Gilbert IH. Azasterols as inhibitors of sterol 24-methyltransferase in Leishmania species and Trypanosoma cruzi. J Med Chem. 2003 Oct 23; 46(22):4714-27. PMID: 14561091.
      View in: PubMed
    97. Dardonville C, Rinaldi E, Hanau S, Barrett MP, Brun R, Gilbert IH. Synthesis and biological evaluation of substrate-based inhibitors of 6-phosphogluconate dehydrogenase as potential drugs against African trypanosomiasis. Bioorg Med Chem. 2003 Jul 17; 11(14):3205-14. PMID: 12818683.
      View in: PubMed
    98. Klenke B, Barrett MP, Brun R, Gilbert IH. Antiplasmodial activity of a series of 1,3,5-triazine-substituted polyamines. J Antimicrob Chemother. 2003 Aug; 52(2):290-3. PMID: 12837742.
      View in: PubMed
    99. Rudyk H, Knaggs MH, Vasiljevic S, Hope J, Birkett C, Gilbert IH. Synthesis and evaluation of analogues of Congo red as potential compounds against transmissible spongiform encephalopathies. Eur J Med Chem. 2003 Jun; 38(6):567-79. PMID: 12832128.
      View in: PubMed
    100. Kirby L, Birkett CR, Rudyk H, Gilbert IH, Hope J. In vitro cell-free conversion of bacterial recombinant PrP to PrPres as a model for conversion. J Gen Virol. 2003 Apr; 84(Pt 4):1013-20. PMID: 12655105.
      View in: PubMed
    101. Dardonville C, Gilbert IH. Synthesis of (R)-2-methyl-4-deoxy and (R)-2-methyl-4,5-dideoxy analogues of 6-phosphogluconate as potential inhibitors of 6-phosphogluconate dehydrogenase. Org Biomol Chem. 2003 Feb 07; 1(3):552-9. PMID: 12926259.
      View in: PubMed
    102. Jimenez Bueno G, Klimkait T, Gilbert IH, Simons C. Solid-phase synthesis of diamine and polyamine amino acid derivatives as HIV-1 tat-TAR binding inhibitors. Bioorg Med Chem. 2003 Jan 02; 11(1):87-94. PMID: 12467711.
      View in: PubMed
    103. Boussard C, Doyle VE, Mahmood N, Klimkait T, Pritchard M, Gilbert IH. Design, synthesis and evaluation of peptide libraries as potential anti-HIV compounds, via inhibition of gp120/cell membrane interactions, using the gp120/cd4/fab17 crystal structure. Eur J Med Chem. 2002 Nov; 37(11):883-90. PMID: 12446047.
      View in: PubMed
    104. Chowdhury SF, Guerrero RH, Brun R, Ruiz-Perez LM, Pacanowska DG, Gilbert IH. Synthesis and testing of 5-benzyl-2,4-diaminopyrimidines as potential inhibitors of leishmanial and trypanosomal dihydrofolate reductase. J Enzyme Inhib Med Chem. 2002 Oct; 17(5):293-302. PMID: 12683746.
      View in: PubMed
    105. Gilbert IH. Inhibitors of dihydrofolate reductase in Leishmania and trypanosomes. Biochim Biophys Acta. 2002 Jul 18; 1587(2-3):249-57. PMID: 12084467.
      View in: PubMed
    106. Doyl VE, Klimkait T, Mahmood N, Slater M, Hazen RJ, Gilbert IH. Synthesis of potential anti-HIV GP120 inhibitors using a lysine template. J Enzyme Inhib Med Chem. 2002 Jun; 17(3):175-82. PMID: 12443043.
      View in: PubMed
    107. Barrett MP, Gilbert IH. Perspectives for new drugs against trypanosomiasis and leishmaniasis. Curr Top Med Chem. 2002 May; 2(5):471-82. PMID: 11966468.
      View in: PubMed
    108. Klenke B, Stewart M, Barrett MP, Brun R, Gilbert IH. Synthesis and biological evaluation of s-triazine substituted polyamines as potential new anti-trypanosomal drugs. J Med Chem. 2001 Oct 11; 44(21):3440-52. PMID: 11585449.
      View in: PubMed
    109. Zuccotto F, Zvelebil M, Brun R, Chowdhury SF, Di Lucrezia R, Leal I, Maes L, Ruiz-Perez LM, Gonzalez Pacanowska D, Gilbert IH. Novel inhibitors of Trypanosoma cruzi dihydrofolate reductase. Eur J Med Chem. 2001 May; 36(5):395-405. PMID: 11451529.
      View in: PubMed
    110. Bertelli M, El-Bastawissy E, Knaggs MH, Barrett MP, Hanau S, Gilbert IH. Selective inhibition of 6-phosphogluconate dehydrogenase from Trypanosoma brucei. J Comput Aided Mol Des. 2001 May; 15(5):465-75. PMID: 11394739.
      View in: PubMed
    111. Chowdhury SF, Di Lucrezia R, Guerrero RH, Brun R, Goodman J, Ruiz-Perez LM, Pacanowska DG, Gilbert IH. Novel inhibitors of Leishmanial dihydrofolate reductase. Bioorg Med Chem Lett. 2001 Apr 23; 11(8):977-80. PMID: 11327604.
      View in: PubMed
    112. Klenke B, Gilbert IH. Nitrile reduction in the presence of Boc-protected amino groups by catalytic hydrogenation over palladium-activated Raney-nickel. J Org Chem. 2001 Apr 06; 66(7):2480-3. PMID: 11281791.
      View in: PubMed
    113. Morgan J, Joyce-Menekse ME, Rowlands RT, Gilbert IH, Lloyd D. Rapid and sensitive quantitation of antibiotics in fermentations by electrospray mass spectrometry. Rapid Commun Mass Spectrom. 2001; 15(14):1229-38. PMID: 11445907.
      View in: PubMed
    114. el-Bastawissy E, Knaggs MH, Gilbert IH. Molecular dynamics simulations of wild-type and point mutation human prion protein at normal and elevated temperature. J Mol Graph Model. 2001; 20(2):145-54. PMID: 11775001.
      View in: PubMed
    115. Knaggs MH, McGuigan C, Harris SA, Heshmati P, Cahard D, Gilbert IH, Balzarini J. A QSAR study investigating the effect of L-alanine ester variation on the anti-HIV activity of some phosphoramidate derivatives of d4T. Bioorg Med Chem Lett. 2000 Sep 18; 10(18):2075-8. PMID: 10999474.
      View in: PubMed
    116. Khabnadideh S, Tan CL, Croft SL, Kendrick H, Yardley V, Gilbert IH. Squalamine analogues as potential anti-trypanosomal and anti-leishmanial compounds. Bioorg Med Chem Lett. 2000 Jun 05; 10(11):1237-9. PMID: 10866389.
      View in: PubMed
    117. Di Lucrezia R, Gilbert IH, Floyd CD. Solid phase synthesis of purines from pyrimidines. J Comb Chem. 2000 May-Jun; 2(3):249-53. PMID: 10827932.
      View in: PubMed
    118. Rudyk H, Vasiljevic S, Hennion RM, Birkett CR, Hope J, Gilbert IH. Screening Congo Red and its analogues for their ability to prevent the formation of PrP-res in scrapie-infected cells. J Gen Virol. 2000 Apr; 81(Pt 4):1155-64. PMID: 10725446.
      View in: PubMed
    119. Chowdhury SF, Villamor VB, Guerrero RH, Leal I, Brun R, Croft SL, Goodman JM, Maes L, Ruiz-Perez LM, Pacanowska DG, Gilbert IH. Design, synthesis, and evaluation of inhibitors of trypanosomal and leishmanial dihydrofolate reductase. J Med Chem. 1999 Oct 21; 42(21):4300-12. PMID: 10543874.
      View in: PubMed
    120. Siddiqui AQ, McGuigan C, Ballatore C, Zuccotto F, Gilbert IH, De Clercq E, Balzarini J. Design and synthesis of lipophilic phosphoramidate d4T-MP prodrugs expressing high potency against HIV in cell culture: structural determinants for in vitro activity and QSAR. J Med Chem. 1999 Oct 07; 42(20):4122-8. PMID: 10514282.
      View in: PubMed
    121. Zuccotto F, Brun R, Gonzalez Pacanowska D, Ruiz Perez LM, Gilbert IH. The structure-based design and synthesis of selective inhibitors of Trypanosoma cruzi dihydrofolate reductase. Bioorg Med Chem Lett. 1999 May 17; 9(10):1463-8. PMID: 10360757.
      View in: PubMed
    122. Goldring AO, Balzarini J, Gilbert IH. Design and synthesis of bio-isosteres of thymidine triphosphate. Bioorg Med Chem Lett. 1998 May 19; 8(10):1211-4. PMID: 9871737.
      View in: PubMed
    123. Zuccotto F, Martin AC, Laskowski RA, Thornton JM, Gilbert IH. Dihydrofolate reductase: a potential drug target in trypanosomes and leishmania. J Comput Aided Mol Des. 1998 May; 12(3):241-57. PMID: 9749368.
      View in: PubMed
    124. Tye CK, Kasinathan G, Barrett MP, Brun R, Doyle VE, Fairlamb AH, Weaver R, Gilbert IH. An approach to use an unusual adenosine transporter to selectively deliver polyamine analogues to trypanosomes. Bioorg Med Chem Lett. 1998 Apr 07; 8(7):811-6. PMID: 9871546.
      View in: PubMed
    125. Moarefi IF, Small D, Gilbert I, Höpfner M, Randall SK, Schneider C, Russo AA, Ramsperger U, Arthur AK, Stahl H, et al. Mutation of the cyclin-dependent kinase phosphorylation site in simian virus 40 (SV40) large T antigen specifically blocks SV40 origin DNA unwinding. J Virol. 1993 Aug; 67(8):4992-5002. PMID: 8392624; PMCID: PMC237887.
    Gilbert's Networks
    Click the "See All" links for more information and interactive visualizations!
    Concepts Expand Description
    _
    Co-Authors Expand Description
    _
    Similar People Expand Description
    _
    Same Department Expand Description