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作为5-羟色胺2C抑制剂的二芳基取代吡咯烷酮和吡咯酮：合成与生物学评价

Diaryl substituted pyrrolidinones and pyrrolones as 5-HT2C inhibitors: synthesis and biological evaluation.

作者信息

Micheli Fabrizio, Pasquarello Alessandra, Tedesco Giovanna, Hamprecht Dieter, Bonanomi Giorgio, Checchia Anna, Jaxa-Chamiec Albert, Damiani Federica, Davalli Silvia, Donati Daniele, Gallotti Chiara, Petrone Marcella, Rinaldi Marilisa, Riley Graham, Terreni Silvia, Wood Martyn

机构信息

GlaxoSmithKline Psychiatry Centre of Excellence for Drug Discovery, Via Fleming, 4, 37135 Verona, Italy.

出版信息

Bioorg Med Chem Lett. 2006 Aug 1;16(15):3906-12. doi: 10.1016/j.bmcl.2006.05.034. Epub 2006 May 30.

DOI:10.1016/j.bmcl.2006.05.034
PMID:16730983
Abstract

Within the continuous quest for the discovery of novel compounds able to treat anxiety and depression, the generation of a pharmacophore model for 5-HT2C receptor antagonists and the discovery of a new class of potent and selective 5-HT2C molecules are reported.

摘要

在持续不断地探索能够治疗焦虑和抑郁的新型化合物的过程中，本文报道了5-HT2C受体拮抗剂药效团模型的构建以及一类新型强效且选择性的5-HT2C分子的发现。

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