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Discovery of novel selective GPR120 agonists with potent anti-diabetic activity by hybrid design.
- Source :
-
Bioorganic & Medicinal Chemistry Letters . Aug2018, Vol. 28 Issue 15, p2599-2604. 6p. - Publication Year :
- 2018
-
Abstract
- GPR120 is an attractive target for the treatment of type 2 diabetes. In this study, a series of biphenyl derivatives were designed, synthesized by hybrid design. The selected compound 6a exhibited potent GPR120 agonist activity (EC 50 = 93 nM) and high selectivity over GPR40. The results of oral glucose tolerance test (OGTT) demonstrated that 6a exhibited significant glucose-lowering effect in glucose-loaded ICR male mice. Analysis of the structure–activity relationship is also presented. Compound 6a deserves further biological evaluation and structural modifications. [ABSTRACT FROM AUTHOR]
- Subjects :
- *CIRCUMCELLIONS
*TYPE 2 diabetes
*GLUCOSE
*BROMODEOXYURIDINE
*UBIQUITINATION
Subjects
Details
- Language :
- English
- ISSN :
- 0960894X
- Volume :
- 28
- Issue :
- 15
- Database :
- Academic Search Index
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Publication Type :
- Academic Journal
- Accession number :
- 131071134
- Full Text :
- https://doi.org/10.1016/j.bmcl.2018.06.047