Synthesis and SAR studies of very potent imidazopyridine antiprotozoal agents.
Basic Information
ID: ALA1146986
Journal: Bioorg Med Chem Lett
Title: Synthesis and SAR studies of very potent imidazopyridine antiprotozoal agents.
Authors: Biftu T, Feng D, Fisher M, Liang GB, Qian X, Scribner A, Dennis R, Lee S, Liberator PA, Brown C, Gurnett A, Leavitt PS, Thompson D, Mathew J, Misura A, Samaras S, Tamas T, Sina JF, McNulty KA, McKnight CG, Schmatz DM, Wyvratt M.
Abstract: Compounds 10a (IC50 110 pM) and 21 (IC50 40 pM) are the most potent inhibitors of Eimeria tenella cGMP-dependent protein kinase activity reported to date and are efficacious in the in vivo antiparasitic assay when administered to chickens at 12.5 and 6.25 ppm levels in the feed. However, both compounds are positive in the Ames microbial mutagenesis assay which precludes them from further development as antiprotozoal agents in the absence of negative lifetime rodent carcinogenicity studies.
CiteXplore: 16464591
DOI: 10.1016/j.bmcl.2006.01.092
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