Synthesis and structure–activity relationship of novel lactam-fused chroman derivatives having dual affinity at the 5-HT 1A receptor and the serotonin transporter

…, DA Evrard, W Childers, BL Harrison, M Chlenov…

Index: Shen, Zhongqi; Siva Ramamoorthy; Hatzenbuhler, Nicole T.; Evrard, Deborah A.; Childers, Wayne; Harrison, Boyd L.; Chlenov, Michael; Hornby, Geoffrey; Smith, Deborah L.; Sullivan, Kelly M.; Schechter, Lee E.; Andree, Terrance H. Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 1 p. 222 - 227

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Citation Number: 11

Abstract

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.