1243675-48-0Relevant articles and documents
Spiroindane based amides as potent and selective MC4R agonists for the treatment of obesity
He, Shuwen,Ye, Zhixiong,Dobbelaar, Peter H.,Sebhat, Iyassu K.,Guo, Liangqin,Liu, Jian,Jian, Tianying,Lai, Yingjie,Franklin, Christopher L.,Bakshi, Raman K.,Dellureficio, James P.,Hong, Qingmei,Weinberg, David H.,MacNeil, Tanya,Tang, Rui,Strack, Alison M.,Tamvakopoulos, Constantin,Peng, Qianping,Miller, Randy R.,Stearns, Ralph A.,Chen, Howard Y.,Chen, Airu S.,Fong, Tung M.,Wyvratt Jr., Matthew J.,Nargund, Ravi P.
experimental part, p. 4399 - 4405 (2010/10/02)
We report a series of potent and selective MC4R agonists based on spiroindane amide privileged structures for potential treatments of obesity. Among the synthetic methods used, Method C allows rapid synthesis of the analogs. The series of compounds can afford high potency on MC4R as well as good rodent pharmacokinetic profiles. Compound 1r (MK-0489) demonstrates MC4R mediated reduction of food intake and body weight in mouse models. Compound 1r is efficacious in 14-day diet-induced obese (DIO) rat models.
