Two analogues of fenarimol show curative activity in an experimental model of chagas disease

M. Keenan; J.H. Chaplin; P.W. Alexander; M.J. Abbott; W. M. Best; A. Khong; A. Botero Gomez; C.J. Perez; S. Cornwall; R.C.A. Thompson; K.L. White; D.M. Shackleford; M. Koltun; F.C.K. Chiu; J. Morizzi; E. Ryan; M. Campbell; T.W. von Geldern; I. Scandale; E. Chatelain; S.A. Charman

doi:10.1021/jm401610c

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Two analogues of fenarimol show curative activity in an experimental model of chagas disease

Journal article

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Two analogues of fenarimol show curative activity in an experimental model of chagas disease

M. Keenan, J.H. Chaplin, P.W. Alexander, M.J. Abbott, W. M. Best, A. Khong, A. Botero Gomez, C.J. Perez, S. Cornwall, R.C.A. Thompson, …

Journal of Medicinal Chemistry, Vol.56(24), pp.10158-10170

2013

DOI: https://doi.org/10.1021/jm401610c

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Abstract

Chagas disease, caused by the protozoan parasite Trypanosoma cruzi (T. cruzi), is an increasing threat to global health. Available medicines were introduced over 40 years ago, have undesirable side effects, and give equivocal results of cure in the chronic stage of the disease. We report the development of two compounds, 6 and (S)-7, with PCR-confirmed curative activity in a mouse model of established T. cruzi infection after once daily oral dosing for 20 days at 20 mg/kg 6 and 10 mg/kg (S)-7. Compounds 6 and (S)-7 have potent in vitro activity, are noncytotoxic, show no adverse effects in vivo following repeat dosing, are prepared by a short synthetic route, and have druglike properties suitable for preclinical development

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Title: Two analogues of fenarimol show curative activity in an experimental model of chagas disease
Authors/Creators: M. Keenan (Author/Creator) - Murdoch University
J.H. Chaplin (Author/Creator) - Murdoch University
P.W. Alexander (Author/Creator) - Murdoch University
M.J. Abbott (Author/Creator) - Murdoch University
W. M. Best (Author/Creator) - Murdoch University
A. Khong (Author/Creator) - Murdoch University
A. Botero Gomez (Author/Creator)
C.J. Perez (Author/Creator) - Murdoch University
S. Cornwall (Author/Creator) - Murdoch University
R.C.A. Thompson (Author/Creator) - Murdoch University
K.L. White (Author/Creator) - Monash University
D.M. Shackleford (Author/Creator) - Monash University
M. Koltun (Author/Creator) - Monash University
F.C.K. Chiu (Author/Creator) - Monash University
J. Morizzi (Author/Creator) - Monash University
E. Ryan (Author/Creator) - Monash University
M. Campbell (Author/Creator) - Monash University
T.W. von Geldern (Author/Creator) - Drugs for Neglected Diseases Initiative
I. Scandale (Author/Creator) - Drugs for Neglected Diseases Initiative
E. Chatelain (Author/Creator) - Drugs for Neglected Diseases Initiative
S.A. Charman (Author/Creator) - Monash University
Publication Details: Journal of Medicinal Chemistry, Vol.56(24), pp.10158-10170
Publisher: American Chemical Society
Identifiers: 991005541015607891
Copyright: © 2013 American Chemical Society.
Murdoch Affiliation: School of Veterinary and Life Sciences
Language: English
Resource Type: Journal article

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Collaboration types: International collaboration
Citation topics: 1 Clinical & Life Sciences; 1.261 Parasitology - Trypanosoma & Leishmania; 1.261.596 Trypanosoma Biology
Web Of Science research areas: Chemistry, Medicinal
ESI research areas: Chemistry