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  • Title: 2-Alkyl-4-aryl-pyrimidine fused heterocycles as selective 5-HT2A antagonists.
    Author: Shireman BT, Dvorak CA, Rudolph DA, Bonaventure P, Nepomuceno D, Dvorak L, Miller KL, Lovenberg TW, Carruthers NI.
    Journal: Bioorg Med Chem Lett; 2008 Mar 15; 18(6):2103-8. PubMed ID: 18282705.
    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-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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