Synthesis and SAR studies of very potent imidazopyridine antiprotozoal agents

…, GB Liang, X Qian, A Scribner, R Dennis, S Lee…

文献索引：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 Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 9 p. 2479 - 2483 Title/Abstract Full Text View citing articles Show Details Feng, Dennis; Fisher, Michael; Liang, Gui-Bai; Qian, Xiaoxia; Brown, Chris; Gurnett, Anne; Leavitt, Penny Sue; Liberator, Paul A.; Mathew, John; Misura, Andrew; Samaras, Samantha; Tamas, Tamas; Schmatz, Dennis M.; Wyvratt, Matthew; Biftu, Tesfaye Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 23 p. 5978 - 5981

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被引用次数: 55

摘要

Compounds 10a (IC50 110pM) and 21 (IC50 40pM) 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 ...