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Design and synthesis of 3-arylpyrrolidine-2-carboxamide derivatives as melanocortin-4 receptor ligands |
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| Authors: | Tran Joe A Tucci Fabio C Arellano Melissa Jiang Wanlong Chen Caroline W Marinkovic Dragan Fleck Beth A Wen Jenny Foster Alan C Chen Chen |
| Affiliation: | Department of Medicinal Chemistry, Neurocrine Biosciences, Inc., 12790 El Camino Real, San Diego, CA 92130, USA. |
| 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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