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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. Among authors: amewu r. 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.
Endoperoxide carbonyl falcipain 2/3 inhibitor hybrids: toward combination chemotherapy of malaria through a single chemical entity.
Gibbons P, Verissimo E, Araujo NC, Barton V, Nixon GL, Amewu RK, Chadwick J, Stocks PA, Biagini GA, Srivastava A, Rosenthal PJ, Gut J, Guedes RC, Moreira R, Sharma R, Berry N, Cristiano ML, Shone AE, Ward SA, O'Neill PM. Gibbons P, et al. Among authors: amewu rk. J Med Chem. 2010 Nov 25;53(22):8202-6. doi: 10.1021/jm1009567. Epub 2010 Oct 27. J Med Chem. 2010. PMID: 20979352
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. Among authors: amewu rk. 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.
Generation of quinolone antimalarials targeting the Plasmodium falciparum mitochondrial respiratory chain for the treatment and prophylaxis of malaria.
Biagini GA, Fisher N, Shone AE, Mubaraki MA, Srivastava A, Hill A, Antoine T, Warman AJ, Davies J, Pidathala C, Amewu RK, Leung SC, Sharma R, Gibbons P, Hong DW, Pacorel B, Lawrenson AS, Charoensutthivarakul S, Taylor L, Berger O, Mbekeani A, Stocks PA, Nixon GL, Chadwick J, Hemingway J, Delves MJ, Sinden RE, Zeeman AM, Kocken CH, Berry NG, O'Neill PM, Ward SA. Biagini GA, et al. Among authors: amewu rk. Proc Natl Acad Sci U S A. 2012 May 22;109(21):8298-303. doi: 10.1073/pnas.1205651109. Epub 2012 May 7. Proc Natl Acad Sci U S A. 2012. PMID: 22566611 Free PMC article.
Synthesis and profiling of benzylmorpholine 1,2,4,5-tetraoxane analogue N205: Towards tetraoxane scaffolds with potential for single dose cure of malaria.
O' Neill PM, Stocks PA, Sabbani S, Roberts NL, Amewu RK, Shore ER, Aljayyoussi G, Angulo-Barturén I, Belén M, Jiménez-Díaz, Bazaga SF, Martínez MS, Campo B, Sharma R, Charman SA, Ryan E, Chen G, Shackleford DM, Davies J, Nixon GL, Biagini GA, Ward SA. O' Neill PM, et al. Among authors: amewu rk. Bioorg Med Chem. 2018 Jul 15;26(11):2996-3005. doi: 10.1016/j.bmc.2018.05.006. Epub 2018 May 17. Bioorg Med Chem. 2018. PMID: 29779669
Two-step synthesis of achiral dispiro-1,2,4,5-tetraoxanes with outstanding antimalarial activity, low toxicity, and high-stability profiles.
Ellis GL, Amewu R, Sabbani S, Stocks PA, Shone A, Stanford D, Gibbons P, Davies J, Vivas L, Charnaud S, Bongard E, Hall C, Rimmer K, Lozanom S, Jesús M, Gargallo D, Ward SA, O'Neill PM. Ellis GL, et al. Among authors: amewu r. J Med Chem. 2008 Apr 10;51(7):2170-7. doi: 10.1021/jm701435h. Epub 2008 Mar 15. J Med Chem. 2008. PMID: 18341274
Synthesis, in vitro and in vivo antimalarial assessment of sulfide, sulfone and vinyl amide-substituted 1,2,4-trioxanes prepared via thiol-olefin co-oxygenation (TOCO) of allylic alcohols.
Amewu R, Gibbons P, Mukhtar A, Stachulski AV, Ward SA, Hall C, Rimmer K, Davies J, Vivas L, Bacsa J, Mercer AE, Nixon G, Stocks PA, O'Neill PM. Amewu R, et al. Org Biomol Chem. 2010 May 7;8(9):2068-77. doi: 10.1039/b924319d. Epub 2010 Mar 3. Org Biomol Chem. 2010. PMID: 20401383 Free article.
36 results