1410798-67-2Relevant academic research and scientific papers
Synthesis and biological evaluation of thienopyrimidine derivatives as GPR119 agonists
Jeon, Moon-Kook,Lee, Kyu Myung,Kim, Il Hyang,Jang, Yoon Kyung,Kang, Seung Kyu,Lee, Jun Mi,Jung, Kwan-Young,Kumar, Jaladi Ashok,Rhee, Sang Dal,Jung, Won Hoon,Song, Jin Sook,Bae, Myung Ae,Kim, Kwang Rok,Ahn, Jin Hee
, p. 4281 - 4285 (2014)
A series of thienopyrimidine derivatives was synthesized and evaluated for their GPR119 agonistic ability. Several thienopyrimidine derivatives containing R1 and R2 substituents displayed potent GPR119 agonistic activity. Among them, compound 5d, which is a prototype, showed good in vitro activity with an EC50 value of 3 nM and human and rat liver microsomal stability. Compound 5d exhibited no CYP inhibition and induction, Herg binding, or mutagenic potential. Compound 5d showed increase insulin secretion in beta TC-6 cell and lowered the glucose excursion in mice in an oral glucose-tolerance test.
