Letters in Drug Design & Discovery

Author(s): B. Rezessy and S. Solyom

DOI: 10.2174/1570180043398948

Advanced Pharmacophore Model of Non-Competitive AMPA Antagonist 2,3-benzodiazepines

Page: [217 - 223] Pages: 7

  • * (Excluding Mailing and Handling)

Abstract

Detailed SAR examination and DIStance COmparison (DISCO) computation were used for identification and superposition of common structural features of 2,3-benzodiazepines with high affinity to an allosteric AMPA binding site. Two similar 4-point models were identified; both contained 2 donor sites, a donor atom and a hydrophobic centre. At one of the donor sites a characteristic difference between the two models was observed.

Keywords: non-competitive ampa antagonist,, 2,3-benzodiazepines, pharmacophore model, disco