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Clobazam: chemical aspects of the 1,4 and 1,5-benzodiazepines (1979)

Clobazam: chemical aspects of the 1,4 and 1,5-benzodiazepines (1979)

  1. Jatelka
    British Journal of Clinical Pharmacology 1979;7 Suppl 1:17S-21S

    Kuch H

    1 The structures and chemistry of the 1,4- and 1,5-benzodiazepines are compared. These two groups of drugs differ in respect to basicity, lipophilicity and electronic charge distribution.

    2 The 1,4-benzodiazepine diazepam has a weakly basic imine group in contrast to the acid methylene protons of clobazam.

    3 The imine function of diazepam is more lipophilic than the carboxamide group of clobazam with its rather hydrophilic character.

    4 Diazepam and clobazam differ in electronic charge distribution and hence in the location of the chemically reactive centres, the imine partial structure in diazepam and the malonic acid portion of clobazam.

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Recent Reviews

  1. Piglet
    Piglet
    5/5,
    Version: 2008-10-30
    An excellent find. The actual routes to the 1,4 & 1,5 benzos are showing their age but the actual discussion of electronic character is a classic.

    Highly recommended for experts and people wanting a deeper understanding of the benzos.