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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. J Med Chem. 2012 May 10;55(9):4189-204. doi: 10.1021/jm2015809. Epub 2012 Apr 27. J Med Chem. 2012. PMID: 22536986
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. 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: keenan m. 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. 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.
A new era for chagas disease drug discovery?
Keenan M, Chaplin JH. Keenan M, et al. Prog Med Chem. 2015;54:185-230. doi: 10.1016/bs.pmch.2014.12.001. Epub 2015 Jan 17. Prog Med Chem. 2015. PMID: 25727705 Review.
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: keenan m. 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
DNDI-6174 is a preclinical candidate for visceral leishmaniasis that targets the cytochrome bc1.
Braillard S, Keenan M, Breese KJ, Heppell J, Abbott M, Islam R, Shackleford DM, Katneni K, Crighton E, Chen G, Patil R, Lee G, White KL, Carvalho S, Wall RJ, Chemi G, Zuccotto F, González S, Marco M, Deakyne J, Standing D, Brunori G, Lyon JJ, Castañeda-Casado P, Camino I, Martinez Martinez MS, Zulfiqar B, Avery VM, Feijens PB, Van Pelt N, Matheeussen A, Hendrickx S, Maes L, Caljon G, Yardley V, Wyllie S, Charman SA, Chatelain E. Braillard S, et al. Among authors: keenan m. Sci Transl Med. 2023 Dec 13;15(726):eadh9902. doi: 10.1126/scitranslmed.adh9902. Epub 2023 Dec 13. Sci Transl Med. 2023. PMID: 38091406 Free PMC article.
390 results