Synthetic and computer-assisted analyses of the pharmacophore for the benzodiazepine receptor inverse agonist site.

@article{Allen1990SyntheticAC,
  title={Synthetic and computer-assisted analyses of the pharmacophore for the benzodiazepine receptor inverse agonist site.},
  author={Michael S Allen and Yong Cheng Tan and Mark L. Trudell and Kuthirummal Narayanan and L R Schindler and M Justina Mart{\'i}n and Carsten Schultz and T. H. J. J. van der Hagen and Konrad F. Koehler and Penelope W Codding},
  journal={Journal of medicinal chemistry},
  year={1990},
  volume={33 9},
  pages={2343-57}
}
The structural requirements for ligand binding to the benzodiazepine receptor (BzR) inverse agonist site were probed through the synthesis and in vitro evaluation of 3-substituted beta-carbolines 6, 7, 11, 12, gamma-carboline 13, and diindoles 18-21, 23-25, 27, 28, and 34. On the basis of the apparent binding affinities of these and other analogues, a hydrogen bond acceptor site (A2) on the receptor is proposed to interact with the N(9) hydrogen atom of the beta-carbolines or the N(7) hydrogen… CONTINUE READING

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