Two Analogues of Fenarimol Show Curative Activity in an Experimental Model of Chagas Disease | Zendy

Martine Keenan | Zendy; Jason H. Chaplin | Zendy; Paul W. Alexander | Zendy; Michael J. Abbott | Zendy; Wayne M. Best | Zendy; Andrea Khong | Zendy; Adriana Botero | Zendy; Catherine Perez | Zendy; Scott Cornwall | Zendy; RC Andrew Thompson | Zendy; Karen L. White | Zendy; David M. Shackleford | Zendy; Maria Koltun | Zendy; Francis C. K. Chiu | Zendy; Julia Morizzi | Zendy; Eileen Ryan | Zendy; Michael G. Campbell | Zendy; Thomas W von Geldern | Zendy; Ivan Scandale | Zendy; Eric Chatelain | Zendy; Susan A. Charman | Zendy

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Two Analogues of Fenarimol Show Curative Activity in an Experimental Model of Chagas Disease

Author(s) -

Martine Keenan,

Jason H. Chaplin,

Paul W. Alexander,

Michael J. Abbott,

Wayne M. Best,

Andrea Khong,

Adriana Botero,

Catherine Perez,

Scott Cornwall,

RC Andrew Thompson,

Karen L. White,

David M. Shackleford,

Maria Koltun,

Francis C. K. Chiu,

Julia Morizzi,

Eileen Ryan,

Michael G. Campbell,

Thomas W von Geldern,

Ivan Scandale,

Eric Chatelain,

Susan A. Charman

Publication year - 2013

Publication title -

journal of medicinal chemistry

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 2.01

H-Index - 261

eISSN - 1520-4804

pISSN - 0022-2623

DOI - 10.1021/jm401610c

Subject(s) - chagas disease , trypanosoma cruzi , dosing , in vivo , pharmacology , chemistry , in vitro , disease , adverse effect , protozoan parasite , parasite hosting , immunology , medicine , biology , biochemistry , microbiology and biotechnology , world wide web , computer science

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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