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Synthesis and biological evaluation of 1, 2, 4‐oxadiazole derivatives as novel GPR119 agonists
Author(s) -
Fu Suhong,
Xiang Wei,
Chen Jinying,
Ma Liang,
Chen Lijuan
Publication year - 2017
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/cbdd.12890
Subject(s) - oxadiazole , chemistry , agonistic behaviour , ec50 , agonist , in vitro , combinatorial chemistry , biochemistry , organic chemistry , receptor , medicine , psychiatry , aggression
A series of 1, 2, 4‐oxadiazole derivatives have been designed and synthesized, and 25 compounds were evaluated their abilities by the assay of cAMP concentration in GPR119‐transfected HEK293T cells. All compounds showed acceptable agonistic effects on GPR119. Among these compounds, 4p exhibited the best agonistic effects with the EC 50 of 20.6 n m , which was comparable to that of positive control GPR119 agonist GSK1292263. The agonistic activity of these 1,2,4‐oxadiazole derivatives led to the establishment of a structure–activity relationship.