Privileged structure based ligands for melanocortin-4 receptors—Aliphatic piperazine derivatives

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.

Different substituted cyclic aliphatic piperazines provide useful privileged structures for the construction of ligands with affinity for melanocortin 4 receptors.Figure optionsDownload as PowerPoint slide