Structure-Activity Relationships of Substituted 2,3,4,4a,5,10b-Hexahydro-benz[h]isoquinoline-6(1H)-ones as 5-HT2C Receptor Antagonists

Authors

  • Heinz Stadler
  • Jürgen Wichmann
  • Andrew J. Sleight
  • Michael Bös

DOI:

https://doi.org/10.2533/chimia.2000.669

Keywords:

5-ht2c receptor antagonists, O-methylasparvenone, Pharmaceutical chemistry, Serotonin, Stereoselective synthesis

Abstract

A series of cis and trans configured 2,3,4,4a,5,10b-hexahydro-benz[h]isoquinoline-6(1H)-ones 2 were studied with respect to the binding affinity to the 5-HT2 subtype receptors. The influence of substituents in positions 7(R1), 8(R2) and 9(R3) on affinity and selectivity to 5-HT2A and 5-HT2C receptors and the preference of one diastereoisomer is discussed.

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Published

2000-11-29

Issue

Vol. 54 No. 11 (2000): Pharmaceutical Chemistry

Section

Scientific Articles

License

Copyright (c) 2000 Swiss Chemical Society

Creative Commons License

This work is licensed under a Creative Commons Attribution-NonCommercial 4.0 International License.

How to Cite

[1]
Chimia 2000, 54, 669, DOI: 10.2533/chimia.2000.669.