gilbert Publications

Publications

2005| 2004| 2003| 2002| 2001| 2000| 1999| 1998| 1997| 1996| 1990-1995

2005

59. Interaction of Monobenzamidine-Linked Trypanocides with the Trypanosoma brucei P2 Aminopurine Transporter, Stewart, M. L.; Boussard, C.; Brun, R.; Gilbert, I. H.; Barrett, M. P. Antimicrob. Agents Chemother. 2005, 49, 5169-5171.

58. Effects of Inhibitors of [Delta]24(25)-Sterol Methyl Transferase on the Ultrastructure of Epimastigotes of Trypanosoma cruzi. Braga, M. V.; Magaraci, F.; Orenes Lorente, S.; Gilbert, I.; de Souza, W. Microscopy & Microanalysis, 2005, 11, 506-511.

57. Analogs of Thiolactomycin as Potential Antimalarial Agents. Jones, S. M.; Urch, J. E.; Kaiser, M.; Brun, R.; Harwood, J. L.; Berry, C.; Gilbert, I. H. J. Med. Chem.,2005, 48, 5932-5941.

56. Deoxyuridine Triphosphate Nucleotidohydrolase as a Potential Antiparasitic Drug Target. Nguyen, C.; Kasinathan, G.; Leal-Cortijo, I.; Musso-Buendia, A.; Kaiser, M.; Brun, R.; Ruiz-Pérez, L. M.; Johansson, N. G.; González-Pacanowska, D.; Gilbert, I. H. J. Med. Chem., 2005, 48, 5942-5954.

55. Design and synthesis of a series of melamine-based nitroheterocycles with activity against trypanosomatid parasites. B aliani, A.; Jimenez Bueno, G.; Stewart, M. L.; Yardley, V.; Brun, R.; Barrett, M. P.; Gilbert, I. H. J. Med. Chem., 2005, 48, 5570-5579.

54. Preparation of Transition-State Analogues of Sterol 24-Methyl Transferase as Potential Anti-Parasitics. Orenes Lorente, S.; Jimenez Jimenez, C.; Gros, L.; Yardley, V.; de Luca-Fradley, K.; Croft, S. L.; Urbina, J. A.; Ruiz-Perez, L. M.; Gonzalez Pacanowska, D.; Gilbert, I. H. Bioorg. Med. Chem ., 2005, 13, 5435-5453.

53. Biphenylquinuclidines as inhibitors of squalene synthase and growth of parasitic protozoa. Orenes Lorente, S.; Gomez, R.; Jimenez, C.; Cammerer, S.; Yardley, V.; de Luca-Fradley, K.; Croft, S. L.; Ruiz Perez, L. M.; Urbina, J.; Gonazalez Pacanowska, D.; Gilbert, I. H. Bioorg. Med. Chem., 2005 , 13, 3519-3529

52. dUTPase as a Platform for Antimalarial Drug Design: Structural Basis for the Selectivity of a Class of Nucleoside Inhibitors. Whittingham, J. L.; Leal, I.; Nguyen, C.; Kasinathan, G.; Bell, E.; Jones, A. F.; Berry, C.; Benito, A.; Turkenburg, J. P.; Dodson, E. J.; Ruiz Perez, L. M.; Wilkinson, A. J.; Johansson, N. G.; Brun, R.; Gilbert, I. H.; Gonzalez Pacanowska, D.; Wilson, K. S. Structure, 2005, 13, 329-338

51. Design, synthesis and evaluation of 2,4-diaminoquinazolines as inhibitors of trypanosomal and leishmanial dihydrofolate reductase. Khabnadideh, S.; Pez, D.; Musso, A.; Brun, R.; Ruiz Pérez, L. M.; González-Pacanowska, D.; Gilbert, I. H. Bioorg. Med. Chem., 2005, 13, 2637-2649

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2004

50. Synthesis of Analogues of Congo Red and Evaluation of Their Anti-Prion Activity. Sellarajah, S.; Lekishvili, T.; Bowring, C.; Thompsett, A. R.; Rudyk, H.; Birkett, C. R.; Brown D. R.; Gilbert, I. H. Journal of Medicinal Chemistry, 2004, 47, 5515-5534

49. Selective inhibition of Trypanosoma brucei 6-phosphogluconate dehydrogenase by high energy intermediate and transition state analogues. Christophe Dardonville, Eliana Rinaldi, Michael P. Barrett, Reto Brun, Ian H. Gilbert and Stefania Hanau. Journal of Medicinal Chemistry, 2004, 47, 3427-3437.

48. Novel Azasterols as Potential Agents for the Treatment of Leishmaniasis and Trypanosomiasis. Silvia Orenes Lorente, Juliany C. F. Rodrigues, Carmen Jiménez Jiménez, Miranda Joyce-Menekse, Carlos Rodrigues, Simon L. Croft, Vanessa Yardley, Kate de Luca-Fradley, Luis M. Ruiz-Pérez, Julio Urbina, Wanderley de Souza, Dolores González Pacanowska and Ian H. Gilbert. Antimicrobial Agents and Chemotherapy , 2004, 48, 1733-1738.

47. Design, Synthesis and Evaluation of Potential Inhibitors of HIV gp120-CD4 Interactions. Cyrille Boussard, Thomas Klimkait, Naheed Mahmood, Martin Pritchard and Ian H. Gilbert Bioorganic and Medicinal Chemistry Letters, 2004, 14, 2673-2676.

46. 6-phosphogluconate dehydrogenase: a target for drugs in African trypanosomes. Stefania Hanau, Eliana Rinaldi, Franco Dallocchio, Ian H. Gilbert, Christophe Dardonville, Margaret J. Adams, Sheila Gover, Michael P. Barrett Current Medicinal Chemistry, 2004, 11 2639-2650.

45. Trypanocidal activity of melamine–based nitroheterocycles. Mhairi L. Stewart, Gorka Jimenez Bueno, Alessandro Baliani , Burkhard Klenke , Reto Brun, Janice M. Brock, Ian H. Gilbert, Michael P. Barrett , Antimicrobial Agents and Chemotherapy, 2004, in press.

44. Analogues of Thiolactomycin as Potential Anti-malarial and Anti-trypanosomal Agents. Simon M. Jones, Jonathan E. Urch, Reto Brun, John L. Harwood, Colin Berry, Ian H. Gilbert. Bioorganic and Medicinal Chemistry, 2004, 12, 683-692.

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2003

43. 2,4-Diaminopyrimidines as Inhibitors of Leishmanial and Trypanosomal Dihydrofolate Reductase. Didier Pez, Isabel Leal, Fabio Zuccotto, Cyrille Boussard, Reto Brun, Simon L. Croft, Vanessa Yardley, Luis M. Ruiz Perez, Dolores Gonzalez Pacanowska and Ian H. Gilbert. Bioorganic and Medicinal Chemistry, 2003, 11, 4693-4711.

42. Azasterols as Inhibitors of Sterol 24-Methyltransferase in Leishmania and Trypanosoma cruzi. Filippo Magaraci, Carmen Jimenez Jimenez, Carlos Rodrigues, Juliany C.F.Rodrigues, Marina Vianna Braga, Vanessa Yardley, Kate de Luca-Fradley, Simon L. Croft, Wanderley de Souza, Luis M. Ruiz-Perez, Julio Urbina, Dolores Gonzalez Pacanowska, and Ian H. Gilbert. Journal of Medicinal Chemistry, 2003, 46, 4714-4727.

41. Anti-Plasmodial activity of a series of 1,3,5 triazine substituted polyamines. Burkhard Klenke, Michael P. Barrett, Reto Brun and Ian H. Gilbert. Journal of AntimicrobialChemotherapy, 2003, 52 , 290-293 .

40. Synthesis and biological evaluation of substrate-based inhibitors of 6-phosphogluconate dehydrogenase as potential drugs against African Trypanosomiasis. Christophe Dardonville, Eliana Rinaldi, Stefania Hanau , Michael P. Barrett , Reto Brun and Ian H. Gilbert, Bioorganic and Medicinal Chemistry, 2003, 11, 3205-3214.

39. Synthesis and Evaluation of Analogues of Congo Red as Potential Compounds against Transmissible Spongiform Encephalopathies. Hélène Rudyk, Michael H. Knaggs, Snezana Vasiljevic, James Hope , Chris Birkett and Ian H. Gilbert. European Journal of Medicinal Chemistry, 2003, 38, 567-579.

38. 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. Christophe Dardonville and Ian H. Gilbert, Organic and Biomolecular Chemistry, 2003, 1, 552-559

37. In vitro cell-free conversion of bacterial recombinant PrP to PrPres as a model for conversion. Louise Kirby, Christopher R Birkett, Helene Rudyk, Ian H Gilbert, James Hope, Journal of General Virology, 2003, 84 , 1013-1020 .

36. Solid-Phase Synthesis of Diamine and Polyamine Amino Acid Derivatives as HIV-1 Tat-TAR Binding Inhibitors. G Jimenez Bueno, T Klimkait, I H Gilbert and C Simons, Bioorganic and Medicinal Chemistry, 2003,11, 87-94.

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2002

35. 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. Cyrille Boussard, Valerie E. Doyle, Naheed Mahmood, Thomas Klimkait, Martyn Pritchard & Ian H. Gilbert. European Journal of Medicinal Chemistry,2002, 37, 883-890.

34. Synthesis And Testing Of 5-Benzyl-2,4-Diaminopyrimidines As Potential Inhibitors Of Leishmanial And Trypanosomal Dihydrofolate Reductase. Shafinaz F. Chowdhury, Ramon Hurtado Guerrero, Reto Brun, Luis M. Ruiz-Perez, Dolores Gonzalez Pacanowska, and Ian H. Gilbert. Journal of Enzyme Inhibition and Medicinal Chemistry , 2002, 17, 293-302.

33. Synthesis of Potential Anti-HIV GP120 Inhibitors Using a Lysine Template V E Doyle, T Klimkait, N Mahmood , M Slater, R J Hazen and I H Gilbert, Journal of Enzyme Inhibition and Medicinal Chemistry, 2002, 17, 175-182.

32. Inhibitors of Dihydrofolate Reductase in Leishmania and Trypanosomes. I. H. Gilbert, Biochimica et Biophysica Acta - Molecular Basis of Disease, 2002, 1587, 249-257.

31. Perspectives for New Drugs against Trypanosomasis and Leishmaniasis. M. P. Barrett and I. H. Gilbert, Current Topics in Medicinal Chemistry, 2002, 2, 471-482.

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2001

30. Synthesis and Biological Evaluation of s-Triazine Substituted Polyamines as Potential New Anti-Trypanosomal Drugs. B. Klenke, M. Stewart, M. P. Barrett, R. Brun and I. H. Gilbert, Journal of Medicinal Chemistry, 2001, 44, 3440-3452.

29. Molecular dynamics simualtions of wild-type and point mutation human prion protein at normal and elevated temperature. E. El-Bastawissy, M. H. Knaggs and I. H. Gilbert, Journal of Molecular Graphics and Modelling, 2001, 20, 145-154.

28. Novel Inhibitors of Trypanosoma cruzi Dihydrofolate Reductase. F. Zuccotto, M. Zvelebil, R. Brun, S. F. Chowdhury, R. Di Lucrezia, I. Leal, L. Maes, L. M. Ruiz-Perez, D. Gonzalez Pacanowska, and I. H. Gilbert, European Journal of Medicinal Chemistry, 2001, 36, 395-405.

27. Rapid and sensitive quantitation of antibiotics in fermentations by electrospray mass spectrometry. J. Morgan, M. E. Joyce-Menekse, R. T. Rowlands, I. H. Gilbert and D. Lloyd, Rapid Communications in Mass Spectrometry, 2001, 15, 1-10.

26. Nitrogen Reduction in the Presence of Boc-protected amino groups by catalytic hydrogenation over palladium activated Raney-Nickel. B. Klenke, I. H. Gilbert, Journal of Organic Chemistry, 2001, 66, 2480-2483.

25. Selective Inhibition of 6-Phosphogluconate Dehydrogenase from Trypanosoma brucei. M. Bertelli, E. El-Bastawissy, M. H. Knaggs, M. P. Barrett, S. Hanau, I. H. Gilbert, Journal of Computer-Aided Molecular Design, 2001, 15, 467-475.

24. Novel Inhibitors of Leishmanial Dihydrofolate Reductase. S. F. Chowdhury, R. Di Lucrezia, R. Hurtado Guerrero, R. Brun, J. Goodman, L. M. Ruiz-Perez, D. Gonzalez Pacanowska, I. H. Gilbert, Bioorganic and Medicinal Chemistry Letters, 2001, 11, 977-980.

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2000

23. A QSAR study investigating the effect of L-alanine ester variation on the anti-HIV activity of some phosphoramidate derivatives of d4T. M. H. Knaggs, C. McGuigan, S. A. Harris, P. Heshmati, D. Cahard, I. H. Gilbert and J. Balzarini, Bioorganic and Medicinal Chemistry Letters, 2000, 10, 2075-2078.

22. Squalamine analogues as potential anti-trypanosomal and anti-leishmanial compounds. S. Khabnadideh, C. L. Tan, S. L. Croft, H. Kendrick, V. Yardley, I. H. Gilbert, Bioorganic and Medicinal Chemistry Letters, 2000, 10, 1237-1239.

21. Solid Phase Synthesis of Purines from Pyrimidines. R. Di Lucrezia, I. H. Gilbert, C. D. Floyd, Journal of Combinatorial Chemistry,2000, 2, 249-253.

20. Screening Congo Red and it is analogues for their ability to prevent the formation of PrP-res in scrapie-infected cell.

H. Rudyk, S. Vasiljevic, R. M. Hennion, C. R. Birkett, J. Hope, I. H. Gilbert, Journal of General Virology, 2000, 81, 1155-1164.

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1999

19. Design, Synthesis and Evaluation of Inhibitors of Trypanosomal and Leishmanial Dihydrofolate Reductase. S. F. Chowdhury, V. Bernier Villamor, R. Hurtado Guerrero, I. Leal, R. Brun, S. L. Croft, J. M. Goodman, L. Maes, L. M. Ruiz-Perez, D. Gonzalez Pacanowska, and I. H. Gilbert, Journal of Medicinal Chemistry, 1999, 42 , 4300-4312 .

18. The 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. A. Siddiqui, C. McGuigan, I.H. Gilbert, C. Ballatore, F. Zuccotto, E. De Clercq, and J. Balzarini, Journal of Medicinal Chemistry, 1999,42, 4122-4128.

17. Inhibitors of Protease-Resistant Prion Formation. I. H. Gilbert and H. Rudyk, International Antiviral News, 1999, 7, 78-82.

16. The Structure-Based Design And Synthesis Of Selective Inhibitors Of Trypanosoma Cruzi Dihydrofolate Reductase. F. Zuccotto, R. Brun, D. Gonzalez Pacanowska, L. M. Ruiz Perez, I. H. Gilbert, Bioorganic and Medicinal Chemistry Letters, 1999, 9, 1463-1468.

15. General Synthesis of 3-Phosphorylated myo-Inositol Phospholipids and Their Derivatives. G. F. Painter, S. J. A. Grove, I. H. Gilbert, A. B. Holmes, P. R. Raithby, M. L. Hill, P. T. Hawkins, L. R. Stephens. Journal of the Chemical Society, Perkin Transactions 1, 1999, 923-936.

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1998

14. Design And Synthesis Of Bio-Isosteres Of Thymidine Triphosphate. A. O. Goldring, J. Balzarini and I. H. Gilbert, Bioorganic and Medicinal Chemistry Letters, 1998, 8, 1211-1215.

13. An Approach To Use An Unusual Adenosine Transporter To Selectively Deliver Polyamine Analogues To Trypanosomes. C.-K. Tye, G. Kasinathan, M. P. Barrett, R. Brun, V. E. Doyle, A. H. Fairlamb, R. Weaver and I. H. Gilbert, Bioorganic and Medicinal Chemistry Letters, 1998, 8, 811-816.

12. Electrospray Mass Spectrometry For Assay of Erythromycin A Extracted From Fermentation Liquor. J. Morgan, R. T. Rowlands, M. E. Joyce-Menekse, I. H. Gilbert, D. Lloyd, Biotechnology Techniques, 1998, 12, 435-438.

11. Dihydrofolate Reductase: a Potential Drug Target in Trypanosomes and Leishmania. F. Zuccotto, A. C. R. Martin, R. A. Laskowski, J. M. Thornton, I. H. Gilbert, Journal of Computer-Aided Molecular Design, 1998, 12, 241-257.

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1997

10. Versatile Synthesis of myo-Inositol Phospholipid Precursors. S. J. A. Grove, I. H. Gilbert, A. B. Holmes, G. F. Painter, M. L. Hill, Journal of the Chemical Society, Chemical Communications, 1997, 1633-1634.

9. The Design and Synthesis of Nucleoside Triphosphate Isosteres as Potential Inhibitors of HIV Reverse Transcriptase. R. Weaver, I. H. Gilbert, Tetrahedron, 1997, 53, 5537-5562.

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1996

8. Lipophilic Bioisosteres of Nucleoside Triphosphates. O. Goldring, I. H. Gilbert, N. Mahmood, J. Balzarini, Bioorganic and Medicinal Chemistry Letters, 1996, 6, 2411-2416.

7. Isosteres of Nucleoside Triphosphates. R. Weaver, I. H. Gilbert, N. Mahmood, J. Balzarini, Bioorganic and Medicinal Chemistry Letters, 1996, 6, 2405-2410.

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1990-95

6. Synthesis of b -Keto and ab -Unsaturated N-Acetylcysteamine Thioesters. I. H. Gilbert, M. Ginty, J. A. O'Neill, T. J. Simpson, J. Staunton and C. L. Willis, Bioorganic and Medicinal Chemistry Letters, 1995, 5, 1587-1590.

5. Imidazolines as Amide Bond Replacements. I. H. Gilbert, D. C. Rees, A. K. Crockett, R. C. F. Jones, Tetrahedron, 1995, 51, 6315-6335.

4. Synthesis of a Homochiral Alpha, Alpha-Disubstituted Alpha, Beta-Diamino-Acid. R. C. F. Jones, A. K. Crockett, D. C. Rees and I. H. Gilbert,Tetrahedron Asymmetry, 1994, 5, 1661-1664.

3. Lewis Acid Catalysed rearrangements of myo-inositol orthoformate derivatives. I. H. Gilbert, A. B. Holmes, M. J. Pestchanker and R. C. Young, Carbohydrate Research,1992, 234, 117-130.

2. Amide bond replacements: incorporation of a 2,5,5-trisubstituted imidazoline into dipeptides and into a CCK-4 derivative.I. H. Gilbert, D. C. Rees and R. S. Richardson, Tetrahedron Letters,1991, 32, 2277-2280.

1. Synthesis of Protected myo-Inositols. I. H. Gilbert, A. B. Holmes and R. C. Young, Tetrahedron Letters,1990, 31, 2633-2634.

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