New Features in Synthesis of Talampanel Related 2,3-Benzodiazepines

S.      Solyom; I.      Pallagi; G.      Abraham; M.      Kertesz; G.      Horvath; P.      Berzsenyi

doi:10.2174/1573406054864133

Abstract

Analogues of talampanel (1), a highly active AMPA antagonist 2,3-benzodiazepine, were synthesized, where the characteristic amino-function was either transposed or sterically shielded. For the key intermediates (hemiketals 6a, b) a new synthetic method of different mechanism was developed. The inactivity of several new compounds indicates the significance of the 4-amino(phenyl) function in BDZs of type 1.

Keywords: oxidation, isochromane, hemiketal, benzodiazepine, metabolism

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Medicinal Chemistry

Title: New Features in Synthesis of Talampanel Related 2,3-Benzodiazepines

Volume: 1 Issue: 5

Author(s): S. Solyom, I. Pallagi, G. Abraham, M. Kertesz, G. Horvath and P. Berzsenyi

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Keywords: oxidation, isochromane, hemiketal, benzodiazepine, metabolism

Abstract: Analogues of talampanel (1), a highly active AMPA antagonist 2,3-benzodiazepine, were synthesized, where the characteristic amino-function was either transposed or sterically shielded. For the key intermediates (hemiketals 6a, b) a new synthetic method of different mechanism was developed. The inactivity of several new compounds indicates the significance of the 4-amino(phenyl) function in BDZs of type 1.

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Solyom S., Pallagi I., Abraham G., Kertesz M., Horvath G. and Berzsenyi P., New Features in Synthesis of Talampanel Related 2,3-Benzodiazepines, Medicinal Chemistry 2005; 1 (5) . https://dx.doi.org/10.2174/1573406054864133