期刊
ACS MEDICINAL CHEMISTRY LETTERS
卷 5, 期 4, 页码 384-389出版社
AMER CHEMICAL SOC
DOI: 10.1021/ml4005123
关键词
GPR40; FFAI; full agonist; insulin secretagoue; type 2 diabetes
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.
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