| Literature DB >> 16464591 |
Tesfaye Biftu1, Dennis Feng, Michael Fisher, Gui-Bai Liang, Xiaoxia Qian, Andrew Scribner, Richard Dennis, Shuliang Lee, Paul A Liberator, Chris Brown, Anne Gurnett, Penny S Leavitt, Donald Thompson, John Mathew, Andrew Misura, Samantha Samaras, Tamas Tamas, Joseph F Sina, Kathleen A McNulty, Crystal G McKnight, Dennis M Schmatz, Matthew Wyvratt.
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.Entities:
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Year: 2006 PMID： 16464591 DOI： 10.1016/j.bmcl.2006.01.092
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823