Studies toward the discovery of the next generation of antidepressants. Part 5: 3,4-Dihydro-2H-benzo[1,4]oxazine derivatives with dual 5-HT1A receptor and serotonin transporter affinity

Dahui Zhou; Boyd L Harrison; Uresh Shah; Terrance H Andree; Geoffrey A Hornby; Rosemary Scerni; Lee E Schechter; Deborah L Smith; Kelly M Sullivan; Richard E Mewshaw

doi:10.1016/j.bmcl.2005.11.054

Studies toward the discovery of the next generation of antidepressants. Part 5: 3,4-Dihydro-2H-benzo[1,4]oxazine derivatives with dual 5-HT1A receptor and serotonin transporter affinity

Bioorg Med Chem Lett. 2006 Mar 1;16(5):1338-41. doi: 10.1016/j.bmcl.2005.11.054. Epub 2005 Dec 5.

Authors

Dahui Zhou¹, Boyd L Harrison, Uresh Shah, Terrance H Andree, Geoffrey A Hornby, Rosemary Scerni, Lee E Schechter, Deborah L Smith, Kelly M Sullivan, Richard E Mewshaw

Affiliation

¹ Chemical and Screening Sciences, Wyeth Research, CN 8000, Princeton, NJ 08543-8000, USA. zhoud@wyeth.com

PMID: 16332439
DOI: 10.1016/j.bmcl.2005.11.054

Abstract

The design, synthesis, and structure-activity relationship of two novel classes of benzoxazine derivatives with dual selective serotonin reuptake inhibitors and 5-HT(1A) receptor activities are described.

MeSH terms

Animals
Antidepressive Agents / chemical synthesis*
Antidepressive Agents / chemistry
Antidepressive Agents / metabolism*
Antidepressive Agents / pharmacology
Benzoxazines / chemical synthesis
Benzoxazines / chemistry*
Benzoxazines / metabolism*
Benzoxazines / pharmacology
Humans
Molecular Structure
Rats
Receptor, Serotonin, 5-HT1A / metabolism*
Serotonin Plasma Membrane Transport Proteins / metabolism*
Structure-Activity Relationship
Substrate Specificity

Substances

Antidepressive Agents
Benzoxazines
Serotonin Plasma Membrane Transport Proteins
Receptor, Serotonin, 5-HT1A