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Page 1
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
Antimalarial activity of novel pyrrolizidinyl derivatives of 4-aminoquinoline.
Sparatore A, Basilico N, Casagrande M, Parapini S, Taramelli D, Brun R, Wittlin S, Sparatore F. Sparatore A, et al. Among authors: brun r. Bioorg Med Chem Lett. 2008 Jul 1;18(13):3737-40. doi: 10.1016/j.bmcl.2008.05.042. Epub 2008 May 16. Bioorg Med Chem Lett. 2008. PMID: 18538567
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.
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.
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.
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.
Synthesis, biological evaluation, and structure-activity relationships of N-benzoyl-2-hydroxybenzamides as agents active against P. falciparum (K1 strain), Trypanosomes, and Leishmania.
Stec J, Huang Q, Pieroni M, Kaiser M, Fomovska A, Mui E, Witola WH, Bettis S, McLeod R, Brun R, Kozikowski AP. Stec J, et al. Among authors: brun r. J Med Chem. 2012 Apr 12;55(7):3088-100. doi: 10.1021/jm2015183. Epub 2012 Mar 20. J Med Chem. 2012. PMID: 22352841 Free PMC 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. Among authors: brun r. ChemMedChem. 2011 Aug 1;6(8):1357-61. doi: 10.1002/cmdc.201100196. Epub 2011 Jun 20. ChemMedChem. 2011. PMID: 21692184 No abstract available.
794 results