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Re-evaluating pretomanid analogues for Chagas disease: Hit-to-lead studies reveal both in vitro and in vivo trypanocidal efficacy.
Thompson AM, O'Connor PD, Marshall AJ, Francisco AF, Kelly JM, Riley J, Read KD, Perez CJ, Cornwall S, Thompson RCA, Keenan M, White KL, Charman SA, Zulfiqar B, Sykes ML, Avery VM, Chatelain E, Denny WA. Thompson AM, et al. Among authors: chatelain e. Eur J Med Chem. 2020 Dec 1;207:112849. doi: 10.1016/j.ejmech.2020.112849. Epub 2020 Sep 18. Eur J Med Chem. 2020. PMID: 33007723
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.
Catechol pyrazolinones as trypanocidals: fragment-based design, synthesis, and pharmacological evaluation of nanomolar inhibitors of trypanosomal phosphodiesterase B1.
Orrling KM, Jansen C, Vu XL, Balmer V, Bregy P, Shanmugham A, England P, Bailey D, Cos P, Maes L, Adams E, van den Bogaart E, Chatelain E, Ioset JR, van de Stolpe A, Zorg S, Veerman J, Seebeck T, Sterk GJ, de Esch IJ, Leurs R. Orrling KM, et al. Among authors: chatelain e. J Med Chem. 2012 Oct 25;55(20):8745-56. doi: 10.1021/jm301059b. Epub 2012 Oct 8. J Med Chem. 2012. PMID: 22963052
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.
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.
123 results