| 16169215 |
Fisher MJ, Backer RT, Collado I, de Frutos O, Husain S, Hsiung HM, Kuklish SL, Mateo AI, Mullaney JT, Ornstein PL, Paredes CG, O'Brian TP, Richardson TI, Shah J, Zgombick JM, Briner K: Privileged structure based ligands for melanocortin receptors--substituted benzylic piperazine derivatives. Bioorg Med Chem Lett. 2005 Nov 15;15(22):4973-8.
Replacement of the aryl piperazine moiety in compound 1 with a variety of substituted benzylic piperazines (6) yields compounds that afford melanocortin receptor 4 (MCR4) activity. Analogs with ortho substitution on the aromatic ring afforded the highest affinity. Resolution of the stereocenter of the benzylic piperazine based privileged structure revealed that the R-enantiomer was more active. |
6(0,0,1,1) |