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Antitrypanosomal activity of fexinidazole metabolites, potential new drug candidates for Chagas disease.
Bahia MT, Nascimento AF, Mazzeti AL, Marques LF, Gonçalves KR, Mota LW, Diniz Lde F, Caldas IS, Talvani A, Shackleford DM, Koltun M, Saunders J, White KL, Scandale I, Charman SA, Chatelain E. Bahia MT, et al. Among authors: chatelain e. Antimicrob Agents Chemother. 2014 Aug;58(8):4362-70. doi: 10.1128/AAC.02754-13. Epub 2014 May 19. Antimicrob Agents Chemother. 2014. PMID: 24841257 Free PMC article.
In vitro and in vivo experimental models for drug screening and development for Chagas disease.
Romanha AJ, Castro SL, Soeiro Mde N, Lannes-Vieira J, Ribeiro I, Talvani A, Bourdin B, Blum B, Olivieri B, Zani C, Spadafora C, Chiari E, Chatelain E, Chaves G, Calzada JE, Bustamante JM, Freitas-Junior LH, Romero LI, Bahia MT, Lotrowska M, Soares M, Andrade SG, Armstrong T, Degrave W, Andrade Zde A. Romanha AJ, et al. Among authors: chatelain e. Mem Inst Oswaldo Cruz. 2010 Mar;105(2):233-8. doi: 10.1590/s0074-02762010000200022. Mem Inst Oswaldo Cruz. 2010. PMID: 20428688 Free article.
Analogues of fenarimol are potent inhibitors of Trypanosoma cruzi and are efficacious in a murine model of Chagas disease.
Keenan M, Abbott MJ, Alexander PW, Armstrong T, Best WM, Berven B, Botero A, Chaplin JH, Charman SA, Chatelain E, von Geldern TW, Kerfoot M, Khong A, Nguyen T, McManus JD, Morizzi J, Ryan E, Scandale I, Thompson RA, Wang SZ, White KL. Keenan M, et al. Among authors: chatelain e. J Med Chem. 2012 May 10;55(9):4189-204. doi: 10.1021/jm2015809. Epub 2012 Apr 27. J Med Chem. 2012. PMID: 22536986
Pharmacological characterization, structural studies, and in vivo activities of anti-Chagas disease lead compounds derived from tipifarnib.
Buckner FS, Bahia MT, Suryadevara PK, White KL, Shackleford DM, Chennamaneni NK, Hulverson MA, Laydbak JU, Chatelain E, Scandale I, Verlinde CL, Charman SA, Lepesheva GI, Gelb MH. Buckner FS, et al. Among authors: chatelain e. Antimicrob Agents Chemother. 2012 Sep;56(9):4914-21. doi: 10.1128/AAC.06244-11. Epub 2012 Jul 9. Antimicrob Agents Chemother. 2012. PMID: 22777048 Free PMC article.
Design, structure-activity relationship and in vivo efficacy of piperazine analogues of fenarimol as inhibitors of Trypanosoma cruzi.
Keenan M, Alexander PW, Diao H, Best WM, Khong A, Kerfoot M, Thompson RC, White KL, Shackleford DM, Ryan E, Gregg AD, Charman SA, von Geldern TW, Scandale I, Chatelain E. Keenan M, et al. Among authors: chatelain e. Bioorg Med Chem. 2013 Apr 1;21(7):1756-63. doi: 10.1016/j.bmc.2013.01.050. Epub 2013 Jan 31. Bioorg Med Chem. 2013. PMID: 23462713 Free article.
Complexes of Trypanosoma cruzi sterol 14α-demethylase (CYP51) with two pyridine-based drug candidates for Chagas disease: structural basis for pathogen selectivity.
Hargrove TY, Wawrzak Z, Alexander PW, Chaplin JH, Keenan M, Charman SA, Perez CJ, Waterman MR, Chatelain E, Lepesheva GI. Hargrove TY, et al. Among authors: chatelain e. J Biol Chem. 2013 Nov 1;288(44):31602-15. doi: 10.1074/jbc.M113.497990. Epub 2013 Sep 18. J Biol Chem. 2013. PMID: 24047900 Free PMC article.
Two analogues of fenarimol show curative activity in an experimental model of Chagas disease.
Keenan M, Chaplin JH, Alexander PW, Abbott MJ, Best WM, Khong A, Botero A, Perez C, Cornwall S, Thompson RA, White KL, Shackleford DM, Koltun M, Chiu FC, Morizzi J, Ryan E, Campbell M, von Geldern TW, Scandale I, Chatelain E, Charman SA. Keenan M, et al. Among authors: chatelain e. J Med Chem. 2013 Dec 27;56(24):10158-70. doi: 10.1021/jm401610c. Epub 2013 Dec 4. J Med Chem. 2013. PMID: 24304150 Free PMC article.
Chagas disease drug discovery: toward a new era.
Chatelain E. Chatelain E. J Biomol Screen. 2015 Jan;20(1):22-35. doi: 10.1177/1087057114550585. Epub 2014 Sep 22. J Biomol Screen. 2015. PMID: 25245987 Review.
126 results