Acylated derivatives of 1,5-benzodiazepines. Part II.

W Nawrocka, H Liszkiewicz, A Nawojski, M Wilimowski, L Kedzierska-Goździk, J Barczyńska, W Wojewódzki, E Duś, A Szelag, M Rutkowska
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引用次数: 0

Abstract

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.

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1,5-苯二氮卓类药物的酰化衍生物。第二部分。
合成了4-甲基- 1h -四氢-1,5-苯并二氮杂平-2- 1(1)和2-甲基-4-苯基- 1h -四氢-1,5-苯并二氮杂平-2-羧酸乙酯(10)的酰化衍生物,并对其中心活性进行了初步测试。酰基化反应包括-、-不饱和酸氯化物、二羧酸单酯一氯化物和二羧酸二氯化物。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具有抗侵袭作用。
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