氯巴占：1,4-和1,5-苯二氮䓬类的化学特性
Clobazam: chemical aspects of the 1,4 and 1,5-benzodiazepines.
作者信息
Kuch H
出版信息
Br J Clin Pharmacol. 1979;7 Suppl 1(Suppl 1):17S-21S. doi: 10.1111/j.1365-2125.1979.tb04659.x.
Abstract
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.
摘要
- 对1,4 - 苯二氮䓬类和1,5 - 苯二氮䓬类的结构与化学性质进行了比较。这两类药物在碱性、亲脂性和电子电荷分布方面存在差异。2. 1,4 - 苯二氮䓬类药物地西泮有一个弱碱性的亚胺基团，这与氯巴占的酸性亚甲基质子形成对比。3. 地西泮的亚胺官能团比氯巴占具有相当亲水性的羧酰胺基团更具亲脂性。4. 地西泮和氯巴占在电子电荷分布上不同，因此在化学反应中心的位置上也不同，地西泮中的亚胺部分结构和氯巴占中的丙二酸部分。
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2
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