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

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

  • Bioorg Med Chem. 2013 Mar 1;21(5):1349-56. doi: 10.1016/j.bmc.2012.12.013.
Tuan-Anh N Pham 1,  Zunhua Yang,  Yuanying Fang,  Jun Luo,  Jongkook Lee,  Haeil Park
Affiliations

Affiliation

  • 1 College of Pharmacy, Kangwon National University, Chunchon 200-701, Republic of Korea.
PMID: 23357035 DOI: 10.1016/j.bmc.2012.12.013
Abstract

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.

Figures