On August 1, 2017, Koshizawa, Tomoaki; Morimoto, Toshiharu; Watanabe, Gen; Watanabe, Toshiaki; Yamasaki, Nao; Sawada, Yoshikazu; Fukuda, Tomoaki; Okuda, Ayumu; Shibuya, Kimiyuki; Ohgiya, Tadaaki published an article.Application of 98946-18-0 The title of the article was Optimization of a novel series of potent and orally bioavailable GPR119 agonists. And the article contained the following:
We describe the discovery and optimization of a novel series of furo[3,2-d]pyrimidines as G protein-coupled receptor 119 agonists. Agonistic activity of 4 (EC50 = 129 nM) was improved by replacing the intramol. hydrogen bond between the fluorine atom and the aniline hydrogen in the head moiety with a covalent C-C bond to enhance conformational restriction, which consequently gave a lead compound 12 (EC50 = 53 nM). Optimized compound 26, which was identified by the further optimization of 12, exhibited potent activity (EC50 = 42 nM) with improved clearance in liver microsomes and induced a 33% reduction in blood glucose area under the curve at a dose of 10 mg/kg in an oral glucose tolerance test in C57BL/6N mice. The experimental process involved the reaction of tert-Butyl trichloroacetimidate(cas: 98946-18-0).Application of 98946-18-0
The Article related to furo pyrimidine derivative preparation oral gpr119 agonist diabetes, furo[3,2-d]pyrimidine, gpr119 agonists, intramolecular hydrogen bond, restricted conformation, type 2 diabetes mellitus and other aspects.Application of 98946-18-0
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