| 16650763 |
Briner K, Collado I, Fisher MJ, Garcia-Paredes C, Husain S, Kuklish SL, Mateo AI, O'Brien TP, Ornstein PL, Zgombick J, de Frutos O: Privileged structure based ligands for melanocortin-4 receptors--aliphatic piperazine derivatives. Bioorg Med Chem Lett. 2006 Jul 1;16(13):3449-53. Epub 2006 May 2.
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. |
33(0,1,1,3) |