Synthesis and biological evaluation of novel 2,4-disubstituted quinazoline analogues as GPR119 agonists

Pham, Tuan-Anh N.; Yang, Zunhua; Fang, Yuanying; Luo, Jun; Lee, Jongkook; Park, Haeil

doi:10.1016/j.bmc.2012.12.013

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Synthesis and biological evaluation of novel 2,4-disubstituted quinazoline analogues as GPR119 agonists

Pham, Tuan-Anh N.;
Yang, Zunhua;
Fang, Yuanying;
Luo, Jun;
Lee, Jongkook;
외 1명

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초록

GPR119 agonist has emerged as a promising target for the treatment of type 2 diabetes. A series of novel 2,4-disubstituted quinazoline analogues was prepared and evaluated their agonistic activity against human GPR119. The analogues bearing azabicyclic amine substituents (12a, 12c and 12g) exhibited better EC50 values than that of OEA though they appeared to be partial agonists. (C) 2012 Elsevier Ltd. All rights reserved.

키워드

GPR119 agonist; Type 2 diabetes; Quinazoline analogues; Azabicyclic amines; PROTEIN-COUPLED RECEPTOR; DISCOVERY; POTENT; DERIVATIVES; INHIBITORS; LIGANDS; AGENTS

제목: Synthesis and biological evaluation of novel 2,4-disubstituted quinazoline analogues as GPR119 agonists

저자: Pham, Tuan-Anh N.; Yang, Zunhua; Fang, Yuanying; Luo, Jun; Lee, Jongkook; Park, Haeil

DOI: 10.1016/j.bmc.2012.12.013

발행일: 2013-03-01

유형: Article

저널명: Bioorganic & Medicinal Chemistry

권: 21

호: 5

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