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

Joe A. Tran,Fabio C. Tucci,Melissa Arellano,Wanlong Jiang,Caroline W. Chen,Dragan Marinkovic,Beth A. Fleck,Jenny Wen,Alan C. Foster,Chen Chen

Bioorganic & Medicinal Chemistry Letters（2008）

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摘要

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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关键词

Synthesis,Pyrrolidine,Melanocortin-4 receptor,Stereoisomer,Structure–activity relationship

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