Model studies on a synthetically facile series of N-substituted phenyl-N'-pyridin-3-yl ureas leading to 1-(3-pyridylcarbamoyl) indolines that are potent and selective 5-HT(2C/2B) receptor antagonists
A model series of 5-HT2C antagonists have been prepared by rapid parallel synthesis. These N-substituted phenyl-N'-pyridin-3-yl ureas were found to have a range of 5-HT2C receptor affinities and selectivities over the closely related 5-HT2A receptor. Extrapolation of simple SAR, derived from th...
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| Veröffentlicht in: | Bioorganic & medicinal chemistry 1999-12, Vol.7 (12), p.2767-2773 |
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| container_title | Bioorganic & medicinal chemistry |
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| creator | Bromidge, S M Dabbs, S Davies, D T Davies, S Duckworth, D M Forbes, I T Gadre, A Ham, P Jones, G E King, F D Saunders, D V Thewlis, K M Vyas, D Blackburn, T P Holland, V Kennett, G A Riley, G J Wood, M D |
| description | A model series of 5-HT2C antagonists have been prepared by rapid parallel synthesis. These N-substituted phenyl-N'-pyridin-3-yl ureas were found to have a range of 5-HT2C receptor affinities and selectivities over the closely related 5-HT2A receptor. Extrapolation of simple SAR, derived from this set of compounds, to the more active but synthetically more complex 1-(3-pyridylcarbamoyl)indoline series allowed us to target optimal substitution patterns and identify potent and selective 5-HT(2C/2B) antagonists. |
| doi_str_mv | 10.1016/S0968-0896(99)00228-X |
| format | Article |
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| identifier | ISSN: 0968-0896 |
| ispartof | Bioorganic & medicinal chemistry, 1999-12, Vol.7 (12), p.2767-2773 |
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| language | eng |
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| subjects | Animals Humans In Vitro Techniques Kinetics Magnetic Resonance Spectroscopy Models, Chemical Phenylurea Compounds - chemical synthesis Phenylurea Compounds - chemistry Phenylurea Compounds - pharmacology Pyridines - chemical synthesis Pyridines - chemistry Pyridines - pharmacology Receptor, Serotonin, 5-HT2B Receptor, Serotonin, 5-HT2C Receptors, Serotonin - drug effects Receptors, Serotonin - metabolism Serotonin Antagonists - chemical synthesis Serotonin Antagonists - chemistry Serotonin Antagonists - pharmacology Structure-Activity Relationship |
| title | Model studies on a synthetically facile series of N-substituted phenyl-N'-pyridin-3-yl ureas leading to 1-(3-pyridylcarbamoyl) indolines that are potent and selective 5-HT(2C/2B) receptor antagonists |
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