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  • Title: 3,4-Dihydro-2H-benzo[1,4]oxazine derivatives as 5-HT6 receptor antagonists.
    Author: Zhao SH, Berger J, Clark RD, Sethofer SG, Krauss NE, Brothers JM, Martin RS, Misner DL, Schwab D, Alexandrova L.
    Journal: Bioorg Med Chem Lett; 2007 Jun 15; 17(12):3504-7. PubMed ID: 17485206.
    Abstract:
    A series of novel 3,4-dihydro-2H-benzo[1,4]oxazine derivatives has been designed and synthesized as 5-HT(6) receptor antagonists. Many of the compounds displayed subnanomolar affinities for the 5-HT(6) receptor and good brain penetration in rats. The relationship of structure and lipophilicity to hERG inhibition of this series of compounds is discussed.
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