Design, synthesis and biological evaluation of novel 7-azaspiro[3.5]nonane derivatives as GPR119 agonists

Bioorganic & Medicinal Chemistry
Daisuke MatsudaNorikazu Ohtake

Abstract

The design and synthesis of a novel class of 7-azaspiro[3.5]nonane GPR119 agonists are described. In this series, optimization of the right piperidine N-capping group (R2) and the left aryl group (R3) led to the identification of compound 54g as a potent GPR119 agonist. Compound 54g showed a desirable PK profile in Sprague-Dawley (SD) rats and a favorable glucose lowering effect in diabetic rats.

Citations

Oct 28, 2019·Journal of Enzyme Inhibition and Medicinal Chemistry·Yuanying FangRonghua Liu
Feb 6, 2020·Bioorganic & Medicinal Chemistry·Jayanta Dowarah, Ved Prakash Singh
Apr 27, 2021·Expert Opinion on Therapeutic Patents·Huilan LiZunhua Yang
May 29, 2021·Bioorganic Chemistry·Ajay ManaithiyaImran A Khan
Dec 22, 2020·Journal of the American Chemical Society·Yangyang YangTian Qin

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