Synthesis And Structure-Activity Relationship Of Novel Lactam-Fused Chroman Derivatives Having Dual Affinity At The 5-Ht1a Receptor And The Serotonin Transporter

Zhongqi Shen, P. Siva Ramamoorthy,Nicole T. Hatzenbuhler,Deborah A. Evrard,Wayne Childers,Boyd L. Harrison,Michael Chlenov,Geoffrey Hornby,Deborah L. Smith,Kelly M. Sullivan,Lee E. Schechter,Terrance H. Andree

Bioorganic & Medicinal Chemistry Letters（2010）

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摘要

The structure-activity relationship (SAR) for three series of lactam-fused chroman derivatives possessing 3-amino substituents was evaluated. Many compounds exhibited affinities for both the 5-HT1A receptor and the 5-HT transporter. Compounds 45 and 53 demonstrated 5-HT1A antagonist activities in the in vitro cAMP turnover model. (C) 2009 Elsevier Ltd. All rights reserved.

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关键词

Selective serotonin reuptake inhibitors,Central nervous system,Antidepressant,5-HT1A antagonist,Lactam-fused chroman amine derivatives

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