115144-40-6Relevant articles and documents
Discovery of novel selective GPR120 agonists with potent anti-diabetic activity by hybrid design
Sheng, Ren,Yang, Liu,Zhang, Yanchun,Xing, Enming,Shi, Rui,Wen, Xiaoan,Wang, Heyao,Sun, Hongbin
supporting information, p. 2599 - 2604 (2018/07/06)
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 (EC50 = 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.
Silver-mediated fluorination of potassium aryltrifluoroborates with Selectfluor Dedicated to Professor Andrea Vasella on the occasion of his 71st birthday
Dubbaka, Srinivas Reddy,Narreddula, Venkateswara Reddy,Gadde, Satyanarayana,Mathew, Thresen
, p. 9676 - 9681 (2015/01/08)
A simple and practical procedure for the silver-mediated fluorination of aryl- and heteroaryltrifluoroborates with electrophilic fluorine from Selectfluor and LiOH·H2O is presented. The reaction procedure is simple and easy to set up, the process produces fluorinated arenes and heteroarenes in good to excellent yields and a wide range of electronically and structurally diverse substrates are tolerated.