2. Academic Validation
  3. 4-Aminopyrimidine tetrahydronaphthols: a series of novel vanilloid receptor-1 antagonists with improved solubility properties

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

  • Bioorg Med Chem Lett. 2008 Mar 15;18(6):1830-4. doi: 10.1016/j.bmcl.2008.02.022.
Elizabeth M Doherty 1,  Daniel Retz,  Narender R Gavva,  Rami Tamir,  James J S Treanor,  Mark H Norman
Affiliations

Affiliation

  • 1 Department of Chemistry Research and Discovery, One Amgen Center Drive, Thousand Oaks, CA 91320-1799, USA. [email protected]
PMID: 18299195 DOI: 10.1016/j.bmcl.2008.02.022
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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