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American Chemical Society, Journal of Medicinal Chemistry, 13(55), p. 6087-6093, 2012

DOI: 10.1021/jm300286a

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Lead Optimization of Antimalarial Propafenone Analogues

Journal article published in 2012 by David Lowes, Anupam Pradhan, Lalitha V. Iyer, Toufan Parman, Jason Gow, Fangyi Zhu, Anna Furimsky, Andrew Lemoff, W. Armand Guiguemde, Martina Sigal, Julie A. Clark, Emily Wilson, Liang Tang, Michele C. Connelly, Joseph L. DeRisi and other authors.
This paper is available in a repository.
This paper is available in a repository.

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Abstract

Previously reported studies identified analogues of propafenone that had potent antimalarial activity, reduced cardiac ion channel activity, and properties that suggested the potential for clinical development for malaria. Careful examination of the bioavailability, pharmacokinetics, toxicology, and efficacy of this series of compounds using rodent models revealed orally bioavailable compounds that are nontoxic and suppress parasitemia in vivo. Although these compounds possess potential for further preclinical development, they also carry some significant challenges.