2. Academic Validation
  3. 3,4-Dihydro-2H-benzo[1,4]oxazine derivatives as 5-HT6 receptor antagonists

3,4-Dihydro-2H-benzo[1,4]oxazine derivatives as 5-HT6 receptor antagonists

  • Bioorg Med Chem Lett. 2007 Jun 15;17(12):3504-7. doi: 10.1016/j.bmcl.2006.12.093.
Shu-Hai Zhao 1,  Jacob Berger,  Robin D Clark,  Steven G Sethofer,  Nancy E Krauss,  Julie M Brothers,  Renee S Martin,  Dinah L Misner,  Dietmar Schwab,  Ludmila Alexandrova
Affiliations

Affiliation

  • 1 Roche Pharmaceuticals, Medicinal Chemistry, 3431 Hillview Avenue, Palo Alto, CA 94304, USA. shu-hai.zhao@roche.com
PMID: 17485206 DOI: 10.1016/j.bmcl.2006.12.093
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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