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…
Index: 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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Citation Number: 65
Abstract
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 ...
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[Bromidge, Steven M.; Dabbs, Steven; Davies, David T.; Davies, Susannah; Duckworth, D. Malcolm; Forbes, Ian T.; Gaster, Laramie M.; Ham, Peter; Jones, Graham E.; King, Frank D.; Mulholland, Keith R.; Saunders, Damian V.; Wyman, Paul A.; Blaney, Frank E.; Clarke, Stephen E.; Blackburn, Thomas P.; Holland, Vicky; Kennett, Guy A.; Lightowler, Sean; Middlemiss, Derek N.; Trail, Brenda; Riley, Graham J.; Wood, Martyn D. Journal of Medicinal Chemistry, 2000 , vol. 43, # 6 p. 1123 - 1134]