Journal article
Two analogues of fenarimol show curative activity in an experimental model of chagas disease
Journal of Medicinal Chemistry, Vol.56(24), pp.10158-10170
2013
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
Details
- Title
- Two analogues of fenarimol show curative activity in an experimental model of chagas disease
- Authors/Creators
- M. Keenan (Author/Creator) - Murdoch UniversityJ.H. Chaplin (Author/Creator) - Murdoch UniversityP.W. Alexander (Author/Creator) - Murdoch UniversityM.J. Abbott (Author/Creator) - Murdoch UniversityW. M. Best (Author/Creator) - Murdoch UniversityA. Khong (Author/Creator) - Murdoch UniversityA. Botero Gomez (Author/Creator)C.J. Perez (Author/Creator) - Murdoch UniversityS. Cornwall (Author/Creator) - Murdoch UniversityR.C.A. Thompson (Author/Creator) - Murdoch UniversityK.L. White (Author/Creator) - Monash UniversityD.M. Shackleford (Author/Creator) - Monash UniversityM. Koltun (Author/Creator) - Monash UniversityF.C.K. Chiu (Author/Creator) - Monash UniversityJ. Morizzi (Author/Creator) - Monash UniversityE. Ryan (Author/Creator) - Monash UniversityM. Campbell (Author/Creator) - Monash UniversityT.W. von Geldern (Author/Creator) - Drugs for Neglected Diseases InitiativeI. Scandale (Author/Creator) - Drugs for Neglected Diseases InitiativeE. Chatelain (Author/Creator) - Drugs for Neglected Diseases InitiativeS.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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Source: InCites
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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