吡咯烷酮作为具有抗恶病质活性的人促黑素皮质激素-4受体口服生物可利用拮抗剂。
Pyrrolidinones as orally bioavailable antagonists of the human melanocortin-4 receptor with anti-cachectic activity.
作者信息
Tran Joe A, Tucci Fabio C, Jiang Wanlong, Marinkovic Dragan, Chen Caroline W, Arellano Melissa, Markison Stacy, Fleck Beth A, Wen Jenny, White Nicole S, Pontillo Joseph, Saunders John, Marks Daniel, Hoare Sam R, Madan Ajay, Foster Alan C, Chen Chen
机构信息
Department of Medicinal Chemistry, Neurocrine Biosciences Inc, San Diego, CA 92130, USA.
出版信息
Bioorg Med Chem. 2007 Aug 1;15(15):5166-76. doi: 10.1016/j.bmc.2007.05.026. Epub 2007 May 17.
A series of pyrrolidinones derived from phenylalanines were synthesized as potent antagonists of the human melanocortin-4 receptor. These compounds showed high potencies and selectivities, and several of them had good oral bioavailabilities. In addition, 12e demonstrated in vivo efficacy in a murine cachexia model.
合成了一系列源自苯丙氨酸的吡咯烷酮，作为人促黑素皮质激素-4受体的强效拮抗剂。这些化合物表现出高效力和选择性，其中几种具有良好的口服生物利用度。此外，12e在小鼠恶病质模型中显示出体内疗效。
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