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Bioorg Med Chem Lett
; 18(6): 1830-4, 2008 Mar 15.
Article
in English
| MEDLINE
| ID: mdl-18299195
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.