On December 1, 2018, Guo, Bin; Guo, Shimeng; Huang, Jing; Li, Jingya; Li, Jia; Chen, Qian; Zhou, Xianli; Xie, Xin; Yang, Yushe published an article.Product Details of 280752-78-5 The title of the article was Design and optimization of 2,3-dihydrobenzo[b][1,4]dioxine propanoic acids as novel GPR40 agonists with improved pharmacokinetic and safety profiles. And the article contained the following:
GPR40 has become a new potential therapeutic target for the treatment of diabetes due to its role in mediating the enhancement of glucose-stimulated insulin secretion in pancreatic β cells with a low risk of hypoglycemia. As an effort to extend the chem. space and identify structurally distinct GPR40 agonists with improved liver safety, a novel series of fused-ring Ph propanoic acid analogs were designed. Comprehensive structure-activity relationship studies around novel scaffolds were conducted and led to several analogs exhibited potent GPR40 agonistic activities and high selectivity against other fatty acid receptors. Further evaluation of pharmacokinetic (PK) profiles and in vivo efficacy identified compound I with excellent PK properties and significant glucose-lowering efficacy during an oral glucose tolerance test. In addition, compound I displayed lower hepatobiliary transporter inhibition and favorable druggability. All results indicate that compound I is a promising candidate for further development. The experimental process involved the reaction of (6-Bromo-2,3-dihydrobenzo[b][1,4]dioxin-2-yl)methanol(cas: 280752-78-5).Product Details of 280752-78-5
The Article related to dihydrobenzodioxine propanoic acid preparation gpr40 agonist antidiabetic pharmacokinetic profile, 2,3-dihydrobenzo[b][1,4]dioxine, gpr40 agonist, insulin secretion, type 2 diabetes mellitus and other aspects.Product Details of 280752-78-5
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