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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
12
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pubmed:dateCreated |
2000-3-23
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pubmed:abstractText |
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.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Phenylurea Compounds,
http://linkedlifedata.com/resource/pubmed/chemical/Pyridines,
http://linkedlifedata.com/resource/pubmed/chemical/Receptor, Serotonin, 5-HT2B,
http://linkedlifedata.com/resource/pubmed/chemical/Receptor, Serotonin, 5-HT2C,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Serotonin,
http://linkedlifedata.com/resource/pubmed/chemical/Serotonin Antagonists
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pubmed:status |
MEDLINE
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pubmed:month |
Dec
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pubmed:issn |
0968-0896
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pubmed:author |
pubmed-author:BlackburnT PTP,
pubmed-author:BromidgeS MSM,
pubmed-author:DabbsSS,
pubmed-author:DaviesD TDT,
pubmed-author:DaviesSS,
pubmed-author:DuckworthD MDM,
pubmed-author:ForbesI TIT,
pubmed-author:GadreAA,
pubmed-author:HamPP,
pubmed-author:HollandVV,
pubmed-author:JonesG EGE,
pubmed-author:KennettG AGA,
pubmed-author:KingF DFD,
pubmed-author:RileyG JGJ,
pubmed-author:SaundersD VDV,
pubmed-author:ThewlisK MKM,
pubmed-author:VyasDD,
pubmed-author:WoodM DMD
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pubmed:issnType |
Print
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pubmed:volume |
7
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
2767-73
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:10658582-Animals,
pubmed-meshheading:10658582-Humans,
pubmed-meshheading:10658582-Kinetics,
pubmed-meshheading:10658582-Magnetic Resonance Spectroscopy,
pubmed-meshheading:10658582-Models, Chemical,
pubmed-meshheading:10658582-Phenylurea Compounds,
pubmed-meshheading:10658582-Pyridines,
pubmed-meshheading:10658582-Receptor, Serotonin, 5-HT2B,
pubmed-meshheading:10658582-Receptor, Serotonin, 5-HT2C,
pubmed-meshheading:10658582-Receptors, Serotonin,
pubmed-meshheading:10658582-Serotonin Antagonists,
pubmed-meshheading:10658582-Structure-Activity Relationship
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pubmed:year |
1999
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pubmed:articleTitle |
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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pubmed:affiliation |
SmithKline Beecham Pharmaceuticals Discovery Research, New Frontiers Science Park, Harlow, Essex, UK. steve_bromidge-1@sbphrd.com
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pubmed:publicationType |
Journal Article,
In Vitro
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