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Bioorg Med Chem Lett. 2010 Apr 1;20(7):2365-9. doi: 10.1016/j.bmcl.2010.01.107. Epub 2010 Jan 25.

Orally active and brain permeable proline amides as highly selective 5HT2c agonists 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

Brain-penetrable proline amides were developed as 5HT2c agonists with more than 1000-fold binding selectivity against 5HT2b receptor. After medicinal chemistry optimization and SAR studies, orally active proline amides with robust efficacy in a rodent food intake inhibition model were uncovered.

PMID:
20202843
DOI:
10.1016/j.bmcl.2010.01.107
[Indexed for MEDLINE]

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