Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1376790 | Bioorganic & Medicinal Chemistry Letters | 2008 | 5 Pages |
Abstract
8-(6-(4-(Trifluoromethyl)phenyl)pyrimidin-4-ylamino)-1,2,3,4-tetrahydronaphthalen-2-ol (4) and analogs (5–10) were shown to be potent inhibitors of human and rat TRPV1 in vitro with increased solubility over our previous series. Synthesis, SAR, and improvements in metabolic stability and absorption of these compounds are described herein.
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Authors
Elizabeth M. Doherty, Daniel Retz, Narender R. Gavva, Rami Tamir, James J.S. Treanor, Mark H. Norman,