Back to Search
Start Over
Improving the Pharmacokinetics of GPR40/FFA1 Full Agonists
- Source :
- ACS Medicinal Chemistry Letters. 5:384-389
- Publication Year :
- 2014
- Publisher :
- American Chemical Society (ACS), 2014.
-
Abstract
- We recently reported the discovery of a potent GPR40 full agonist AM-1638 (1). Herein, we describe our efforts in improving the drug-like properties of the full agonists through the systematic introduction of polar groups in the C-, D-, and A-rings. This led to the discovery of new GPR40 full agonists with significantly improved pharmacokinetic propeties. Compound 8 and 20 also showed potent in vivo efficacy in oral glucose tolerance tests in mice in addition to the improvement in properties.
Details
- ISSN :
- 19485875
- Volume :
- 5
- Database :
- OpenAIRE
- Journal :
- ACS Medicinal Chemistry Letters
- Accession number :
- edsair.doi.dedup.....06439f1cb4f3cdf9f6fcdb67b8a2cf08
- Full Text :
- https://doi.org/10.1021/ml4005123