444582-15-4Relevant articles and documents
Melanocortin subtype-4 receptor agonists containing a piperazine core with substituted aryl sulfonamides
Fotsch, Christopher,Han, Nianhe,Arasasingham, Premilla,Bo, Yunxin,Carmouche, Michelle,Chen, Ning,Davis, James,Goldberg, Martin H.,Hale, Clarence,Hsieh, Feng-Yin,Kelly, Michael G.,Liu, Qingyian,Norman, Mark H.,Smith, Duncan M.,Stec, Markian,Tamayo, Nuria,Xi, Ning,Xu, Shimin,Bannon, Anthony W.,Baumgartner, James W.
, p. 1623 - 1627 (2007/10/03)
The biological activity for a set of melanocortin-4 receptor (MC4R) agonists containing a piperazine core with an ortho-substituted aryl sulfonamide is described. Compounds from this set had binding and functional activities at MC4R less than 30 nM. The most selective compound in this series was >25,000-fold more potent at MC4R than MC3R, and 490-fold more potent at MC4R than MC5R. This compound also reduced food intake after oral dosing at 25, 50, and 100 mg kg-1 in fasted mice.
Aryl piperazine melanocortin MC4 receptor agonists
Dyck, Brian,Parker, Jessica,Phillips, Teresa,Carter, Lee,Murphy, Brian,Summers, Robin,Hermann, Julia,Baker, Tracy,Cismowski, Mary,Saunders, John,Goodfellow, Val
, p. 3793 - 3796 (2007/10/03)
Incorporation of substituted phenyl piperazine privileged structures into a known MC4 specific dipeptoid consensus sequence resulted in a series of potent (EC50=24 nM) and selective MC4-R agonists. We report the SAR of this series of compounds
