In 2017,Li, Zheng; Liu, Chunxia; Xu, Xue; Qiu, Qianqian; Su, Xin; Dai, Yuxuan; Yang, Jianyong; Li, Huilan; Shi, Wei; Liao, Chen; Pan, Miaobo; Huang, Wenlong; Qian, Hai published 《Discovery of phenylsulfonyl acetic acid derivatives with improved efficacy and safety as potent free fatty acid receptor 1 agonists for the treatment of type 2 diabetes》.European Journal of Medicinal Chemistry published the findings.Name: 1-Bromo-2-isopropylbenzene The information in the text is summarized as follows:
The free fatty acid receptor 1 (FFA1) has emerged as an attractive anti-diabetic target that mediates glucose-stimulated insulin secretion. Several FFA1 agonists have been reported, but many of them possessed somewhat high lipophilicity and/or mol. weight Herein, the authors describe the identification of sulfone-carboxylic acid moiety with the multiple advantages of reducing lipophilicity, cytotoxicity and β-oxidation associated with compound 2 (I). Further structure-activity relationship study based on the privileged scaffolds led to the discovery of 2-{(4-[(2′-chloro-[1,1′-biphenyl]-3-yl)methoxy]phenyl)sulfonyl}acetic acid (compound 20), which showed a better balance than compound 2 in terms of physicochem. properties, cytotoxicity profiles and pharmacokinetic properties. Subsequent in vivo studies demonstrated that compound 20 robustly improves the glucose tolerance both in normal and type 2 diabetic models without the risk of hypoglycemia. Compared to the high risk of TAK-875 induced liver toxicity, there was no significant adverse effects such as hepatic and renal toxicity were observed in the chronic toxicity studies of compound 20 even at the higher dose. The experimental part of the paper was very detailed, including the reaction process of 1-Bromo-2-isopropylbenzene(cas: 7073-94-1Name: 1-Bromo-2-isopropylbenzene)
1-Bromo-2-isopropylbenzene(cas: 7073-94-1) belongs to organobromine compounds.The reactivity of organobromine compounds resembles but is intermediate between the reactivity of organochlorine and organoiodine compounds. Name: 1-Bromo-2-isopropylbenzene The principal reactions for organobromides include dehydrobromination, Grignard reactions, reductive coupling, and nucleophilic substitution.
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary