946399-69-5Relevant articles and documents
Piperazine sulfonamides as potent, selective, and orally available 11β-hydroxysteroid dehydrogenase type 1 inhibitors with efficacy in the rat cortisone-induced hyperinsulinemia model
Xiang, Jason,Wan, Zhao-Kui,Li, Huan-Qiu,Ipek, Manus,Binnun, Eva,Nunez, Jill,Chen, Lihren,McKew, John C.,Mansour, Tarek S.,Xu, Xin,Suri, Vipin,Tam, May,Xing, Yuzhe,Li, Xiangping,Hahm, Seung,Tobin, James,Saiah, Eddine
supporting information; experimental part, p. 4068 - 4071 (2009/05/30)
11β-Hydroxysteroid dehydrogenase type 1 (11β-HSD1) is the enzyme that converts cortisone to cortisol. Evidence suggests that selective inhibition of 11β-HSD1 could treat diabetes and metabolic syndrome. Presented herein are the synthesis, structure-activity relationship, and in vivo evaluation of piperazine sulfonamides as 11β-HSD1 inhibitors. Through modification of our initial lead 5a, we have identified potent and selective 11β-HSD1 inhibitors such as 13q and 13u with good pharmacokinetic properties.
