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Bioorg Med Chem Lett. 2010 Mar 1;20(5):1758-62. doi: 10.1016/j.bmcl.2010.01.043. Epub 2010 Jan 20.

Identification of piperazine-bisamide GHSR antagonists for the treatment of obesity.

Author information

1
Amgen Inc. 1120 Veterans Boulevard, South San Francisco, CA 94080, USA. yum@amgen.com

Abstract

Piperazine-bisamide analogs were discovered as partial agonists of human growth hormone secretagogue receptor (GHSR) in a high throughput screen. The partial agonists were optimized for potency and converted into antagonists through structure-activity relationship (SAR) studies. The efforts also led to the identification of potent antagonist with favorable PK profile suitable as a tool compound for in vivo studies.

PMID:
20137933
DOI:
10.1016/j.bmcl.2010.01.043
[Indexed for MEDLINE]

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