1,5-苯二氮䓬的酰化衍生物。第二部分。
Acylated derivatives of 1,5-benzodiazepines. Part II.
作者信息
Nawrocka W, Liszkiewicz H, Nawojski A, Wilimowski M, Kedzierska-Goździk L, Barczyńska J, Wojewódzki W, Duś E, Szelag A, Rutkowska M
机构信息
Department of Technology of Drugs, Medical Academy, Wrocłøaw, Poland.
出版信息
Pol J Pharmacol Pharm. 1991 Nov-Dec;43(6):495-503.
Acylated derivatives of 4-methyl-1H-tetrahydro-1,5-benzodiazepin-2-one (1) and of 2-methyl-4-phenyl-1H-tetrahydro-1,5-benzodiazepino-2-carboxylic acid ethyl ester (10) were synthesized and preliminarily tested on their central activity. Acylation was carried out with alpha, beta-unsaturated acid chlorides, dicarboxylic acid monoester monochlorides, and dicarboxylic acid dichlorides. Compounds 2, 3, 11 and 12 had analgesic, compounds 4, 11 and 12--anticonvulsant, and compounds 3 and 11--antiaggressive properties.
合成了4-甲基-1H-四氢-1,5-苯并二氮杂卓-2-酮（1）和2-甲基-4-苯基-1H-四氢-1,5-苯并二氮杂卓-2-羧酸乙酯（10）的酰化衍生物，并对其中枢活性进行了初步测试。酰化反应是用α，β-不饱和酰氯、二羧酸单酯单酰氯和二羧酸二酰氯进行的。化合物2、3、11和12具有镇痛作用，化合物4、11和12具有抗惊厥作用，化合物3和11具有抗攻击作用。
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