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. 2014 Sep 1;24(17):4281-5.
doi: 10.1016/j.bmcl.2014.07.020. Epub 2014 Jul 28.

Synthesis and biological evaluation of thienopyrimidine derivatives as GPR119 agonists

Moon-Kook Jeon  1 , Kyu Myung Lee  1 , Il Hyang Kim  1 , Yoon Kyung Jang  2 , Seung Kyu Kang  1 , Jun Mi Lee  1 , Kwan-Young Jung  1 , Jaladi Ashok Kumar  1 , Sang Dal Rhee  1 , Won Hoon Jung  1 , Jin Sook Song  1 , Myung Ae Bae  1 , Kwang Rok Kim  1 , Jin Hee Ahn  3
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Synthesis and biological evaluation of thienopyrimidine derivatives as GPR119 agonists

Moon-Kook Jeon et al. Bioorg Med Chem Lett. .

Abstract

A series of thienopyrimidine derivatives was synthesized and evaluated for their GPR119 agonistic ability. Several thienopyrimidine derivatives containing R(1) and R(2) 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.

Keywords: Diabetes; GPR119; Thienopyrimidine; Treatment.

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