Design and synthesis of 3-arylpyrrolidine-2-carboxamide derivatives as melanocortin-4 receptor ligands

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Abstract

Based on 3-phenylpropionamides, a series of 3-arylpyrrolidine-2-carboxamide derivatives was designed and synthesized to study the effect of cyclizations as melanocortin-4 receptor ligands. It was found that the 2R,3R-pyrrolidine isomer possessed the most potent affinity among the four stereoisomers.

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    Present address: Department of Medicinal Chemistry, Tanabe Research Laboratories, U.S.A., Inc., 4540 Towne Centre Ct., San Diego, CA 92121, USA.

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