The discovery of potent blockers of the canonical transient receptor channels, TRPC3 and TRPC6, based on an anilino-thiazole pharmacophore

…, L Barton, S Manns, A Waszkiewicz, C Pritchard…

文献索引：Washburn, David G.; Holt, Dennis A.; Dodson, Jason; McAtee, Jeff J.; Terrell, Lamont R.; Barton, Linda; Manns, Sharada; Waszkiewicz, Anna; Pritchard, Christina; Gillie, Dan J.; Morrow, Dwight M.; Davenport, Elizabeth A.; Lozinskaya, Irina M.; Guss, Jeffrey; Basilla, Jonathan B.; Negron, Lorena Kallal; Klein, Michael; Willette, Robert N.; Fries, Rusty E.; Jensen, Timothy C.; Xu, Xiaoping; Schnackenberg, Christine G.; Marino Jr., Joseph P. Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 17 p. 4979 - 4984

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被引用次数: 13

摘要

Abstract Lead optimization of piperidine amide HTS hits, based on an anilino-thiazole core, led to the identification of analogs which displayed low nanomolar blocking activity at the canonical transient receptor channels 3 and 6 (TRPC3 & 6) based on FLIPR (carbachol stimulated) and electrophysiology (OAG stimulated) assays. In addition, the anilino-thiazole amides displayed good selectivity over other TRP channels (TRPA1, TRPV1, and TRPV4), ...