Title of article
2-Alkyl-4-aryl-pyrimidine fused heterocycles as selective 5-HT2A antagonists
Author/Authors
Brock T. Shireman، نويسنده , , Curt A. Dvorak، نويسنده , , Dale A. Rudolph، نويسنده , , Pascal Bonaventure، نويسنده , , Diane Nepomuceno، نويسنده , , Lisa Dvorak، نويسنده , , Kirsten L. Miller، نويسنده , , Timothy W. Lovenberg، نويسنده , , Nicholas I. Carruthers، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2008
Pages
6
From page
2103
To page
2108
Abstract
The synthesis and SAR for a novel series of 2-alkyl-4-aryl-tetrahydro-pyrido-pyrimidines and 2-alkyl-4-aryl-tetrahydro-pyrimido-azepines is described. Representative compounds were shown to be subtype selective 5-HT2A antagonists. Optimal placement of a basic nitrogen relative to the pyrimidine and the presence of a 4-fluorophenyl group in the pyrimidine 4-position was found to have a profound effect on affinity and selectivity.
Keywords
5-HT2C , 5-HT2A , 5-HT , 5-HT2B , Serotonin
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2008
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
799307
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