Synthesis and biological evaluation of novel 2,4-disubstituted quinazoline analogues as GPR119 agonists.
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 EC(50) values than that of OEA though they appeared to be partial agonists.
College of Pharmacy, Kangwon National University, Chunchon 200-701, Republic of Korea.
Tuan-Anh N
TA
Pham
Zunhua
Z
Yang
Yuanying
Y
Fang
Jun
J
Luo
Jongkook
J
Lee
Haeil
H
Park
D000588:Amines / Q000737:chemistry; D001372:Aza Compounds / Q000737:chemistry; D001643:Bridged Bicyclo Compounds / Q000737:chemistry; D004353:Drug Evaluation, Preclinical; D006801:Humans; D011485:Protein Binding; D011799:Quinazolines / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism; D043562:Receptors, G-Protein-Coupled / Q000819:agonists* / Q000378:metabolism; D013329:Structure-Activity Relationship
D000588:Amines; D001372:Aza Compounds; D001643:Bridged Bicyclo Compounds; C519854:GPR119 protein, human; D011799:Quinazolines; D043562:Receptors, G-Protein-Coupled