Presumed pharmacophoric groups of melanocortin peptides (naphthalene, amino or guanidine, and indole moieties) were combined in mimetics molecules looking for their favorable location for activity at melanocortin (MC) receptors. Twenty-two compounds were prepared and tested. The best of these displayed micromolar affinities for the MC receptors.
Department of Pharmaceutical Biosciences, Division of Pharmacology, Uppsala Biomedical Center, PO Box 591, Uppsala University, S-751 24 Uppsala, Sweden.