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Candidate selection and preclinical evaluation of N-tert-butyl isoquine (GSK369796), an affordable and effective 4-aminoquinoline antimalarial for the 21st century.
O'Neill PM, Park BK, Shone AE, Maggs JL, Roberts P, Stocks PA, Biagini GA, Bray PG, Gibbons P, Berry N, Winstanley PA, Mukhtar A, Bonar-Law R, Hindley S, Bambal RB, Davis CB, Bates M, Hart TK, Gresham SL, Lawrence RM, Brigandi RA, Gomez-delas-Heras FM, Gargallo DV, Ward SA. O'Neill PM, et al. J Med Chem. 2009 Mar 12;52(5):1408-15. doi: 10.1021/jm8012618. J Med Chem. 2009. PMID: 19222165
Synthesis, antimalarial activity, and preclinical pharmacology of a novel series of 4'-fluoro and 4'-chloro analogues of amodiaquine. Identification of a suitable "back-up" compound for N-tert-butyl isoquine.
O'Neill PM, Shone AE, Stanford D, Nixon G, Asadollahy E, Park BK, Maggs JL, Roberts P, Stocks PA, Biagini G, Bray PG, Davies J, Berry N, Hall C, Rimmer K, Winstanley PA, Hindley S, Bambal RB, Davis CB, Bates M, Gresham SL, Brigandi RA, Gomez-de-Las-Heras FM, Gargallo DV, Parapini S, Vivas L, Lander H, Taramelli D, Ward SA. O'Neill PM, et al. J Med Chem. 2009 Apr 9;52(7):1828-44. doi: 10.1021/jm8012757. J Med Chem. 2009. PMID: 19284751 Free article.
Antimalarial mannoxanes: hybrid antimalarial drugs with outstanding oral activity profiles and a potential dual mechanism of action.
Chadwick J, Amewu RK, Marti F, Garah FB, Sharma R, Berry NG, Stocks PA, Burrell-Saward H, Wittlin S, Rottmann M, Brun R, Taramelli D, Parapini S, Ward SA, O'Neill PM. Chadwick J, et al. ChemMedChem. 2011 Aug 1;6(8):1357-61. doi: 10.1002/cmdc.201100196. Epub 2011 Jun 20. ChemMedChem. 2011. PMID: 21692184 No abstract available.
Identification, design and biological evaluation of bisaryl quinolones targeting Plasmodium falciparum type II NADH:quinone oxidoreductase (PfNDH2).
Pidathala C, Amewu R, Pacorel B, Nixon GL, Gibbons P, Hong WD, Leung SC, Berry NG, Sharma R, Stocks PA, Srivastava A, Shone AE, Charoensutthivarakul S, Taylor L, Berger O, Mbekeani A, Hill A, Fisher NE, Warman AJ, Biagini GA, Ward SA, O'Neill PM. Pidathala C, et al. J Med Chem. 2012 Mar 8;55(5):1831-43. doi: 10.1021/jm201179h. Epub 2012 Feb 24. J Med Chem. 2012. PMID: 22364416 Free PMC article.
Identification, design and biological evaluation of heterocyclic quinolones targeting Plasmodium falciparum type II NADH:quinone oxidoreductase (PfNDH2).
Leung SC, Gibbons P, Amewu R, Nixon GL, Pidathala C, Hong WD, Pacorel B, Berry NG, Sharma R, Stocks PA, Srivastava A, Shone AE, Charoensutthivarakul S, Taylor L, Berger O, Mbekeani A, Hill A, Fisher NE, Warman AJ, Biagini GA, Ward SA, O'Neill PM. Leung SC, et al. J Med Chem. 2012 Mar 8;55(5):1844-57. doi: 10.1021/jm201184h. Epub 2012 Feb 24. J Med Chem. 2012. PMID: 22364417 Free PMC article.
Identification of novel antimalarial chemotypes via chemoinformatic compound selection methods for a high-throughput screening program against the novel malarial target, PfNDH2: increasing hit rate via virtual screening methods.
Sharma R, Lawrenson AS, Fisher NE, Warman AJ, Shone AE, Hill A, Mbekeani A, Pidathala C, Amewu RK, Leung S, Gibbons P, Hong DW, Stocks P, Nixon GL, Chadwick J, Shearer J, Gowers I, Cronk D, Parel SP, O'Neill PM, Ward SA, Biagini GA, Berry NG. Sharma R, et al. J Med Chem. 2012 Apr 12;55(7):3144-54. doi: 10.1021/jm3001482. Epub 2012 Mar 22. J Med Chem. 2012. PMID: 22380711 Free PMC article.
198 results