444893-53-2Relevant academic research and scientific papers
Optimization of privileged structures for selective and potent melanocortin subtype-4 receptor ligands
Hong, Qingmei,Bakshi, Raman K.,Dellureficio, James,He, Shuwen,Ye, Zhixiong,Dobbelaar, Peter H.,Sebhat, Iyassu K.,Guo, Liangqin,Liu, Jian,Jian, Tianying,Tang, Rui,Kalyani, Rubana N.,MacNeil, Tanya,Vongs, Aurawan,Rosenblum, Charles I.,Weinberg, David H.,Peng, Qingping,Tamvakopoulos, Constantin,Miller, Randy R.,Stearns, Ralph A.,Cashen, Doreen,Martin, Willian J.,Chen, Airu S.,Metzger, Joseph M.,Chen, Howard Y.,Strack, Allison M.,Fong, Tung M.,MacLntyre, Euan,Van Der Ploeg, Lex H.T.,Wyvratt, Matthew J.,Nargund, Ravi P.
scheme or table, p. 4483 - 4486 (2010/10/02)
Design, syntheses and structure-activity relationships of N-acetylated piperazine privileged structures containing MC4R agonist compounds were described. The most potent derivatives were low nM MC4R selective full agonists. Several compounds from the series had modest pharmacokinetic properties.
Privileged structure based ligands for melanocortin-4 receptors-Aliphatic piperazine derivatives
Briner, Karin,Collado, Iván,Fisher, Matthew J.,García-Paredes, Cristina,Husain, Saba,Kuklish, Steven L.,Mateo, Ana I.,O'Brien, Thomas P.,Ornstein, Paul L.,Zgombick, John,de Frutos, óscar
, p. 3449 - 3453 (2007/10/03)
Aliphatic carbocyclic replacement of the benzyl group of compound 1 yielded compounds with high affinity for the melanocortin-4 receptor (MC4R). Compounds with a cyclohexyl group showed a consistent high affinity, while different polar groups with less basicity were good replacements for the original diethyl amines. Substitution of the polar group found in these privileged structures with an aliphatic moiety produced compounds with high affinity for MC4R.
