4-Aminopyrimidine tetrahydronaphthols: A series of novel vanilloid receptor-1 antagonists with improved solubility properties

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 absorpti...

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