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.
MeSH terms
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Animals
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CHO Cells
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Cricetinae
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Cricetulus
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Dogs
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Humans
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Pyrimidinones / chemistry*
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Pyrimidinones / pharmacology
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Pyrimidinones / therapeutic use*
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Receptor, Serotonin, 5-HT2B / metabolism
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Receptor, Serotonin, 5-HT2C / metabolism*
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Serotonin 5-HT2 Receptor Agonists*
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Serotonin Receptor Agonists / chemistry*
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Serotonin Receptor Agonists / pharmacology
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Serotonin Receptor Agonists / therapeutic use*
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Structure-Activity Relationship
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Urethra / drug effects
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Urinary Incontinence / drug therapy
Substances
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Pyrimidinones
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Receptor, Serotonin, 5-HT2B
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Receptor, Serotonin, 5-HT2C
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Serotonin 5-HT2 Receptor Agonists
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Serotonin Receptor Agonists