发现1,3-二取代-1H-吡咯衍生物作为强效促黑素细胞激素受体1（MCH-R1）拮抗剂。
Discovery of 1,3-disubstituted-1H-pyrrole derivatives as potent melanin-concentrating hormone receptor 1 (MCH-R1) antagonists.
作者信息
Berglund Susanne, Egner Bryan J, Gradén Henrik, Gradén Joakim, Morgan David G A, Inghardt Tord, Giordanetto Fabrizio
机构信息
Medicinal Chemistry, AstraZeneca R&D Mölndal, Pepparedsleden 1, SE-431 83, Mölndal, Sweden.
出版信息
Bioorg Med Chem Lett. 2008 Sep 1;18(17):4859-63. doi: 10.1016/j.bmcl.2008.07.079. Epub 2008 Jul 24.
A series of 1,3-disubstituted-1H-pyrrole-based antagonists of the human Melanin-Concentrating Hormone Receptor 1 (h-MCH-R1) are reported. High-throughput screening of the AstraZeneca compound collection yielded 1, a hit with moderate affinity towards MCH-R1. Subsequent structural manipulations and SAR analysis served to rationalize potency requirements, and 12 was identified as a novel, functional MCH-R1 antagonist with favorable pharmacokinetic properties.
报道了一系列基于1,3-二取代-1H-吡咯的人类促黑素细胞激素受体1（h-MCH-R1）拮抗剂。对阿斯利康化合物库进行高通量筛选得到了1，它对MCH-R1具有中等亲和力。随后的结构操作和构效关系分析有助于阐明活性要求，并且12被鉴定为一种具有良好药代动力学性质的新型功能性MCH-R1拮抗剂。
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