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Evaluation of novel TGR5 agonist in combination with Sitagliptin for possible treatment of type 2 diabetes.

Abstract：

:TGR5 is a member of G protein-coupled receptor (GPCR) superfamily, a promising molecular target for metabolic diseases. Activation of TGR5 promotes secretion of glucagon-like peptide-1 (GLP-1), which activates insulin secretion. A series of 2-thio-imidazole derivatives have been identified as novel, potent and orally efficacious TGR5 agonists. Compound 4d, a novel TGR5 agonist, in combination with Sitagliptin, a DPP-4 inhibitor, has demonstrated an adequate GLP-1 secretion and glucose lowering effect in animal models, suggesting a potential clinical option in treatment of type-2 diabetes.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Agarwal S,Sasane S,Kumar J,Deshmukh P,Bhayani H,Giri P,Giri S,Soman S,Kulkarni N,Jain M

doi

10.1016/j.bmcl.2018.04.011

subject

Has Abstract

pub_date

2018-06-01 00:00:00

pages

1849-1852

issue

10

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(18)30309-3

journal_volume

28

pub_type

杂志文章

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