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. 2009 Sep 15;19(18):5346-50.
doi: 10.1016/j.bmcl.2009.07.133. Epub 2009 Aug 6.

Design and synthesis of piperazinylpyrimidinones as novel selective 5-HT(2C) agonists

Mark D Andrews  1 , Martin P Green, Charlotte M N Allerton, David V Batchelor, Julian Blagg, Alan D Brown, David W Gordon, Gordon McMurray, Daniel J Millns, Carly L Nichols, Lesa Watson
Affiliations

Design and synthesis of piperazinylpyrimidinones as novel selective 5-HT(2C) agonists

Mark D Andrews et al. Bioorg Med Chem Lett. .

Abstract

This Letter reports the design and synthesis of several novel series of piperazinyl pyrimidinones as 5-HT(2C) agonists. Several of the compounds presented exhibit good in vitro potency and selectivity over the closely related 5-HT(2A) and 5-HT(2B) receptors. Compound 11 was active in in vivo models of stress urinary incontinence.

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