Discovery of 5-methyl-2-(4-((4-(methylsulfonyl)benzyl)oxy)phenyl)-4-(piperazin-1-yl)pyrimidine derivatives as novel GRP119 agonists for the treatment of diabetes and obesity

Discovery of 5-methyl-2-(4-((4-(methylsulfonyl)benzyl)oxy)phenyl)-4-(piperazin-1-yl)pyrimidine... A series of fused-pyrimidine derivatives were prepared and evaluated for their agonistic activities against human GPR119. Compound 9i showed high potent agonistic activity against HEK293T cells over-expressing human GPR119 and improved glucose tolerance in dose-dependent manner, as well as promoted insulin secretion. In a DIO mice model, 9i also ameliorated the obese-related symptoms by decreasing the body weights without markedly changing food intake, normalized some serum biomarkers, such as ALT, AST, ALP, GLU, CHOL, HDL, and LDL, and exerted therapeutic activity on fat deposition in liver tissue. We consider 9i to have utility as a GPR119 agonists for the treatment of type 2 diabetes mellitus and obese-related symptoms. http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png Molecular Diversity Springer Journals

Discovery of 5-methyl-2-(4-((4-(methylsulfonyl)benzyl)oxy)phenyl)-4-(piperazin-1-yl)pyrimidine derivatives as novel GRP119 agonists for the treatment of diabetes and obesity

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/lp/springer_journal/discovery-of-5-methyl-2-4-4-methylsulfonyl-benzyl-oxy-phenyl-4-N9KERzbyRF
Publisher
Springer International Publishing
Copyright
Copyright © 2017 by Springer International Publishing Switzerland
Subject
Life Sciences; Biochemistry, general; Organic Chemistry; Polymer Sciences; Pharmacy
ISSN
1381-1991
eISSN
1573-501X
D.O.I.
10.1007/s11030-017-9755-6
Publisher site
See Article on Publisher Site

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