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Bioorg Med Chem Lett. 2006 Feb;16(3):731-6. Epub 2005 Nov 2.

New bicyclic cannabinoid receptor-1 (CB1-R) antagonists.

Author information

1
Pfizer Global Research and Development-Groton Laboratories, Groton, CT 06340, USA. philip.a.carpino@pfizer.com

Abstract

A series of conformationally constrained bicyclic derivatives derived from SR141716 was prepared and evaluated as hCB(1)-R antagonists and inverse agonists. Optimization of the structure-activity relationships around the 2,6-dihydro-pyrazolo[4,3-d]pyrimidin-7-one derivative 2a led to the identification of two compounds with oral activity in rodent feeding models (2h and 4a). Replacement of the PP group in 2h with other bicyclic groups resulted in a loss of binding affinity.

PMID:
16263283
DOI:
10.1016/j.bmcl.2005.10.019
[Indexed for MEDLINE]

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