Format

Send to

Choose Destination
Bioorg Med Chem Lett. 2010 Jan 1;20(1):266-71. doi: 10.1016/j.bmcl.2009.10.112. Epub 2009 Oct 30.

Design and synthesis of orally-active and selective azaindane 5HT2c agonist for the treatment of obesity.

Author information

1
Pfizer Global Research and Development, Chemistry Department, 10770 Science Center Drive, La Jolla, CA 92120, United States. kevin.k.liu@pfizer.com

Abstract

Based on our original pyrazine hit, CP-0809101, novel conformationally-restricted 5HT2c receptor agonists with 2-piperazin-azaindane scaffold were designed. Synthesis and structure-activity relationship (SAR) studies are described with emphasis on optimization of the selectivity against 5HT2a and 5HT2b receptors with excellent 2c potency. Orally-active and selective compounds were identified with dose-responsive in vivo efficacy in our pre-clinical food intake model.

PMID:
19914063
DOI:
10.1016/j.bmcl.2009.10.112
[Indexed for MEDLINE]

Supplemental Content

Full text links

Icon for Elsevier Science
Loading ...
Support Center