Literature DB >> 28666737

Design, synthesis, and biological evaluation of aryl N-methoxyamide derivatives as GPR119 agonists.

Yoon Kyung Jang1, Kyu Myung Lee1, Kwan-Young Jung1, Seung Kyu Kang1, Suvarna H Pagire1, Jun Mi Lee1, Haushabhau S Pagire1, Kwang Rok Kim1, Myung Ae Bae1, Hohjai Lee2, Sang Dal Rhee1, Jin Hee Ahn3.   

Abstract

A series of N-methoxyamide derivatives was identified and evaluated as GPR119 agonists. Several N-methoxyamides with thienopyrimidine and pyridine scaffolds showed potent GPR119 agonistic activities. Among them, compound 9c displayed good in vitro activity and potency. Moreover, compound 9c lowered glucose excursion in mice in an oral glucose tolerance test and increased GLP-1 secretion in intestinal cells.
Copyright © 2017. Published by Elsevier Ltd.

Entities:  

Keywords:  Diabetes; GPR119; N-methoxyamide derivative; Treatment

Mesh:

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Year:  2017        PMID: 28666737     DOI: 10.1016/j.bmcl.2017.06.032

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  1 in total

1.  Optimisation of novel 4, 8-disubstituted dihydropyrimido[5,4-b][1,4]oxazine derivatives as potent GPR 119 agonists.

Authors:  Yuanying Fang; Shaokun Zhang; Min Li; Lijuan Xiong; Liangxing Tu; Saisai Xie; Yi Jin; Yanhua Liu; Zunhua Yang; Ronghua Liu
Journal:  J Enzyme Inhib Med Chem       Date:  2020-12       Impact factor: 5.051

  1 in total

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