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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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18초록
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
- 발행일
- 2013-03-01
- 유형
- Article
- 권
- 21
- 호
- 5
- 페이지
- 1349 ~ 1356
- 언어
- ENG
- 출판사
- PERGAMON-ELSEVIER SCIENCE LTD
- 발행국가
- 영국
- 분량
- 8 페이지
- ISSN
- E 1464-3391
P 0968-0896