We have discovered a novel series of isothiazole-based phenylpropanoic acids as GPR120 agonists. Extensive structure-activity relationship studies led to the discovery of a potent GPR120 agonist , which displayed good EC values in both calcium and β-arrestin assays. It also presented good pharmaceutical properties and a favorable PK profile. Moreover, it demonstrated antidiabetic activity in C57BL/6 DIO mice. Studies in WT and knockout DIO mice showed that it improved glucose handling during an OGTT via GPR120. Overall, possessed promising antidiabetic effect and good safety profile to be a development candidate.
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5601374 | PMC |
| http://dx.doi.org/10.1021/acsmedchemlett.7b00233 | DOI Listing |
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Discovery of an Isothiazole-Based Phenylpropanoic Acid GPR120 Agonist as a Development Candidate for Type 2 Diabetes.
ACS Med Chem Lett
September 2017
Cardiovascular and Metabolic Research, Janssen Research & Development, LLC, Welsh & McKean Roads, Box 776, Spring House, Pennsylvania 19477, United States.
We have discovered a novel series of isothiazole-based phenylpropanoic acids as GPR120 agonists. Extensive structure-activity relationship studies led to the discovery of a potent GPR120 agonist , which displayed good EC values in both calcium and β-arrestin assays. It also presented good pharmaceutical properties and a favorable PK profile.
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