Novel and selective 5-HT2C/2B receptor antagonists as potential anxiolytic agents: synthesis, quantitative structure-activity relationships, and molecular modeling of …

…, DM Duckworth, IT Forbes, P Ham…

文献索引：Bromidge; Duckworth; Forbes; Ham; King; Thewlis; Blaney; Naylor; Blackburn; Kennett; Wood; Clarke Journal of Medicinal Chemistry, 1997 , vol. 40, # 22 p. 3494 - 3496

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被引用次数: 65

摘要

The synthesis, biological activity, and molecular modeling of a novel series of substituted 1- (3-pyridylcarbamoyl) indolines are reported. These compounds are isosteres of the previously published indole urea 1 (SB-206553) and illustrate the use of aromatic disubstitution as a replacement for fused five-membered rings in the context of 5-HT2C/2B receptor antagonists. By targeting a region of space previously identified as sterically ...