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Updated: Apr 26, 2026

In Vitro Imaging and Quantification of the Drug Targeting Efficiency of Fluorescently Labeled GnRH Analogues
Published on: March 21, 2017
Synthesis and biological evaluation of thienopyrimidine derivatives as GPR119 agonists
Moon-Kook Jeon1, Kyu Myung Lee1, Il Hyang Kim1
1Drug Discovery Division, Korea Research Institute of Chemical Technology, Republic of Korea.
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.
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