2-Alkyl-4-aryl-pyrimidine fused heterocycles as selective 5-HT2A antagonists.

2-Alkyl-4-aryl-pyrimidine fused heterocycles as selective 5-HT2A antagonists. Research Abstract Details 

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2-Alkyl-4-aryl-pyrimidine fused heterocycles as selective 5-HT2A antagonists. Abstract Text:

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-HT(2A) 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.

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2-Alkyl-4-aryl-pyrimidine fused heterocycles as selective 5-HT2A antagonists. Journal Published:

PUBLICATION TYPE: Journal Article

Journal: Bioorganic & medicinal chemistry letters

VOLUME: 18

Page Numbers: 2103-8

Journal Abbreviation: Bioorg. Med. Chem. Lett.

ISSN: 1464-3405

DAY: 30

MONTH: 01

YEAR: 2008

2-Alkyl-4-aryl-pyrimidine fused heterocycles as selective 5-HT2A antagonists. Information

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LANGUAGE: eng

NlmUniqueID: 9107377

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AFFILIATION: Johnson & Johnson Pharmaceutical Research and Development, L.L.C., 3210 Merryfield Row, San Diego, CA 92121, USA. BShirema@prdus.jnj.com <BShirema@prdus.jnj.com>

Country: England

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MEDLINETA: Bioorg Med Chem Lett

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