Design,synthesis, and biological evaluation of aryl N-methoxyamide derivatives as GPR119 agonists |
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| Authors: | Yoon Kyung Jang Kyu Myung Lee Kwan-Young Jung Seung Kyu Kang Suvarna H. Pagire Jun Mi Lee Haushabhau S. Pagire Kwang Rok Kim Myung Ae Bae Hohjai Lee Sang Dal Rhee Jin Hee Ahn |
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| Affiliation: | 1. Drug Discovery Division, Korea Research Institute of Chemical Technology, Daejeon 305-600, Republic of Korea;2. Department of Chemistry, Gwangju Institute of Science and Technology, Gwangju 61005, Republic of Korea |
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| 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. |
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| Keywords: | Diabetes GPR119 Treatment |
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