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Discovery of substituted (4-phenyl-1H-imidazol-2-yl)methanamine as potent somatostatin receptor 3 agonists.

Abstract：

:We report SAR studies on a novel non-peptidic somatostatin receptor 3 (SSTR3) agonist lead series derived from (4-phenyl-1H-imidazol-2-yl)methanamine. This effort led to the discovery of a highly potent low molecular weight SSTR3 agonist 5c (EC50=5.2 nM, MW=359). The results from molecular overlays of 5c onto the L-129 structure indicate good alignment, and two main differences of the proposed overlays of the antagonist MK-4256 onto the conformation of 5c lead to inversion of antagonism to agonism.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Lai Z,He S,Sherer EC,Wu Z,Yu Y,Ball R,Hong Q,Yang DX,Guo L,Li D,Tuang Q,Chicchi GG,Trusca D,Tsao KL,Zhou YP,Howard AD,Nargund RP,Hagmann WK

doi

10.1016/j.bmcl.2015.06.087

subject

Has Abstract

pub_date

2015-09-01 00:00:00

pages

3520-5

issue

17

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(15)00692-7

journal_volume

25

pub_type

杂志文章

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