In 2013,Xia, Guangxin; You, Xiaodi; Liu, Lin; Liu, Haiyan; Wang, Jianfa; Shi, Yufang; Li, Ping; Xiong, Bing; Liu, Xuejun; Shen, Jingkang published 《Design, synthesis and SAR of piperidyl-oxadiazoles as 11β-hydroxysteroid dehydrogenase 1 inhibitors》.European Journal of Medicinal Chemistry published the findings.Related Products of 76006-33-2 The information in the text is summarized as follows:
The potential roles of 11β-HSD1 inhibitors in metabolic syndrome, T2D and obesity were well established and currently several classes of 11β-HSD1 inhibitors have been developed as promising agents against metabolic diseases. To find potent compounds with good pharmacokinetics, the authors used the bioisosterism approach, and designed the compounds I (R = Ph, cyclohexyl) bearing a 1,2,4-oxadiazole ring to replace the amide group in compound II. Guided by docking study, they then transformed compound I (R = phenyl) into a potent lead compound III by changing the sulfonamide group to an amide. To elaborate this series of piperidyl-oxadiazole derivatives as human 11β-HSD1 inhibitors, they explored the structure-activity relationship of several parts of the lead compound Based on their potency toward human 11β-HSD1 two compounds IV (R1 = 2-Me-3-Br-C6H3, cyclohexyl) were advanced to pharmacokinetic study. It was found that compounds IV are potent and selective human 11β-HSD1 inhibitors with better pharmacokinetic properties than those of the original piperidine-3-carboxamide compound II, and suitable for further in vivo preclin. study in primate model. The experimental process involved the reaction of 3-Bromo-2-methylbenzoic acid(cas: 76006-33-2Related Products of 76006-33-2)
3-Bromo-2-methylbenzoic acid(cas: 76006-33-2) belongs to organobromine compounds. A variety of minor organobromine compounds are found in nature, but none are biosynthesized or required by mammals. The most pervasive is the naturally produced bromomethane.Related Products of 76006-33-2
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary