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Synthesis and SAR studies of very potent imidazopyridine antiprotozoal agents |
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| Authors: | Biftu Tesfaye Feng Dennis Fisher Michael Liang Gui-Bai Qian Xiaoxia Scribner Andrew Dennis Richard Lee Shuliang Liberator Paul A Brown Chris Gurnett Anne Leavitt Penny S Thompson Donald Mathew John Misura Andrew Samaras Samantha Tamas Tamas Sina Joseph F McNulty Kathleen A McKnight Crystal G Schmatz Dennis M Wyvratt Matthew |
| Institution: | Merck Research Laboratories, Department of Medicinal Chemistry, Merck and Co., Inc, PO Box 2000, Rahway, NJ 07065, USA. Tesfaye_Biftu@merck.com |
| 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. |
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