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794 results

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Spirotetrahydro beta-carbolines (spiroindolones): a new class of potent and orally efficacious compounds for the treatment of malaria.
Yeung BK, Zou B, Rottmann M, Lakshminarayana SB, Ang SH, Leong SY, Tan J, Wong J, Keller-Maerki S, Fischli C, Goh A, Schmitt EK, Krastel P, Francotte E, Kuhen K, Plouffe D, Henson K, Wagner T, Winzeler EA, Petersen F, Brun R, Dartois V, Diagana TT, Keller TH. Yeung BK, et al. Among authors: brun r. J Med Chem. 2010 Jul 22;53(14):5155-64. doi: 10.1021/jm100410f. J Med Chem. 2010. PMID: 20568778 Free PMC article.
Spiroindolones, a potent compound class for the treatment of malaria.
Rottmann M, McNamara C, Yeung BK, Lee MC, Zou B, Russell B, Seitz P, Plouffe DM, Dharia NV, Tan J, Cohen SB, Spencer KR, González-Páez GE, Lakshminarayana SB, Goh A, Suwanarusk R, Jegla T, Schmitt EK, Beck HP, Brun R, Nosten F, Renia L, Dartois V, Keller TH, Fidock DA, Winzeler EA, Diagana TT. Rottmann M, et al. Among authors: brun r. Science. 2010 Sep 3;329(5996):1175-80. doi: 10.1126/science.1193225. Science. 2010. PMID: 20813948 Free PMC article.
Imidazolopiperazines: hit to lead optimization of new antimalarial agents.
Wu T, Nagle A, Kuhen K, Gagaring K, Borboa R, Francek C, Chen Z, Plouffe D, Goh A, Lakshminarayana SB, Wu J, Ang HQ, Zeng P, Kang ML, Tan W, Tan M, Ye N, Lin X, Caldwell C, Ek J, Skolnik S, Liu F, Wang J, Chang J, Li C, Hollenbeck T, Tuntland T, Isbell J, Fischli C, Brun R, Rottmann M, Dartois V, Keller T, Diagana T, Winzeler E, Glynne R, Tully DC, Chatterjee AK. Wu T, et al. Among authors: brun r. J Med Chem. 2011 Jul 28;54(14):5116-30. doi: 10.1021/jm2003359. Epub 2011 Jun 23. J Med Chem. 2011. PMID: 21644570 Free PMC article.
Imidazolopiperazines: lead optimization of the second-generation antimalarial agents.
Nagle A, Wu T, Kuhen K, Gagaring K, Borboa R, Francek C, Chen Z, Plouffe D, Lin X, Caldwell C, Ek J, Skolnik S, Liu F, Wang J, Chang J, Li C, Liu B, Hollenbeck T, Tuntland T, Isbell J, Chuan T, Alper PB, Fischli C, Brun R, Lakshminarayana SB, Rottmann M, Diagana TT, Winzeler EA, Glynne R, Tully DC, Chatterjee AK. Nagle A, et al. Among authors: brun r. J Med Chem. 2012 May 10;55(9):4244-73. doi: 10.1021/jm300041e. Epub 2012 Apr 23. J Med Chem. 2012. PMID: 22524250 Free PMC article.
Combining 4-aminoquinoline- and clotrimazole-based pharmacophores toward innovative and potent hybrid antimalarials.
Gemma S, Campiani G, Butini S, Joshi BP, Kukreja G, Coccone SS, Bernetti M, Persico M, Nacci V, Fiorini I, Novellino E, Taramelli D, Basilico N, Parapini S, Yardley V, Croft S, Keller-Maerki S, Rottmann M, Brun R, Coletta M, Marini S, Guiso G, Caccia S, Fattorusso C. Gemma S, et al. Among authors: brun r. J Med Chem. 2009 Jan 22;52(2):502-13. doi: 10.1021/jm801352s. J Med Chem. 2009. PMID: 19113955 Free article.
Preclinical evaluation of the antifolate QN254, 5-chloro- N'6'-(2,5-dimethoxy-benzyl)-quinazoline-2,4,6-triamine, as an antimalarial drug candidate.
Nzila A, Rottmann M, Chitnumsub P, Kiara SM, Kamchonwongpaisan S, Maneeruttanarungroj C, Taweechai S, Yeung BK, Goh A, Lakshminarayana SB, Zou B, Wong J, Ma NL, Weaver M, Keller TH, Dartois V, Wittlin S, Brun R, Yuthavong Y, Diagana TT. Nzila A, et al. Among authors: brun r. Antimicrob Agents Chemother. 2010 Jun;54(6):2603-10. doi: 10.1128/AAC.01526-09. Epub 2010 Mar 29. Antimicrob Agents Chemother. 2010. PMID: 20350951 Free PMC article.
Malaria-infected mice are cured by oral administration of new artemisinin derivatives.
Posner GH, Chang W, Hess L, Woodard L, Sinishtaj S, Usera AR, Maio W, Rosenthal AS, Kalinda AS, D'Angelo JG, Petersen KS, Stohler R, Chollet J, Santo-Tomas J, Snyder C, Rottmann M, Wittlin S, Brun R, Shapiro TA. Posner GH, et al. Among authors: brun r. J Med Chem. 2008 Feb 28;51(4):1035-42. doi: 10.1021/jm701168h. Epub 2008 Jan 31. J Med Chem. 2008. PMID: 18232653
Identification of a new chemical class of antimalarials.
Brunner R, Aissaoui H, Boss C, Bozdech Z, Brun R, Corminboeuf O, Delahaye S, Fischli C, Heidmann B, Kaiser M, Kamber J, Meyer S, Papastogiannidis P, Siegrist R, Voss T, Welford R, Wittlin S, Binkert C. Brunner R, et al. Among authors: brun r. J Infect Dis. 2012 Sep 1;206(5):735-43. doi: 10.1093/infdis/jis418. Epub 2012 Jun 25. J Infect Dis. 2012. PMID: 22732921
Optimization of 4-aminoquinoline/clotrimazole-based hybrid antimalarials: further structure-activity relationships, in vivo studies, and preliminary toxicity profiling.
Gemma S, Camodeca C, Sanna Coccone S, Joshi BP, Bernetti M, Moretti V, Brogi S, Bonache de Marcos MC, Savini L, Taramelli D, Basilico N, Parapini S, Rottmann M, Brun R, Lamponi S, Caccia S, Guiso G, Summers RL, Martin RE, Saponara S, Gorelli B, Novellino E, Campiani G, Butini S. Gemma S, et al. Among authors: brun r. J Med Chem. 2012 Aug 9;55(15):6948-67. doi: 10.1021/jm300802s. Epub 2012 Jul 27. J Med Chem. 2012. PMID: 22783984
794 results