Diamine Derivatives as Novel Small-Molecule, Potent, and Subtype-Selective Somatostatin SST3 Receptor Agonists

ACS Med Chem Lett. 2014 Apr 24;5(6):690-5. doi: 10.1021/ml500079u.

Derun Li ¹, Zhicai Wu ¹, Yang Yu ¹, Richard G Ball ¹, Liangqin Guo ¹, Edward Sherer ¹, Shuwen He ¹, Qingmei Hong ¹, Zhong Lai ¹, Hongbo Qi ¹, Quang Truong ¹, David X Yang ¹, Gary G Chicchi ¹, Kwei-Lan Tsao ¹, Dorina Trusca ¹, Maria Trujillo ¹, Michele Pachanski ¹, George J Eiermann ¹, Andrew D Howard ¹, Yun-Ping Zhou ¹, Bei B Zhang ¹, Ravi P Nargund ¹, William K Hagmann ¹

Affiliations

Affiliation

1 Departments of Medicinal Chemistry and Diabetes Research, Merck Research Laboratories , 126 East Lincoln Avenue, Rahway, New Jersey 07065, United States.

PMID: 24944745 DOI: 10.1021/ml500079u

Abstract

A novel class of small-molecule, highly potent, and subtype-selective somatostatin SST3 agonists was discovered through modification of a SST3 antagonist. As an example, (1R,2S)-9 demonstrated not only potent in vitro SST3 agonist activity but also in vivo SST3 agonist activity in a mouse oral glucose tolerance test (OGTT). These agonists may be useful reagents for studying the physiological roles of the SST3 receptor and may potentially be useful as therapeutic agents.

Keywords

GPCR; Somatostatin; small-molecule SST3 agonists; somatostin receptor subtype 3 (SST3).

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