Synthesis and Analgesic and Anticonvulsant Activity of 4-Substituted 2,2-Dialkyl-1,2-Dihydrobenzo [f] Isoquinolinium Chlorides

被引：1
作者：
Mikhailovskii, A. G. [1 ]
Gashkova, O., V [1 ]
Rudakova, I. P. [1 ]
Chashchina, S., V [1 ]
机构：
[1] Perm State Pharmaceut Acad, Perm 614990, Russia
来源：
PHARMACEUTICAL CHEMISTRY JOURNAL | 2020年 / 53卷 / 11期
关键词：
Ritter cyclocondensation; 2-(1-naphthyl)-1; 1-(R-1)(2)-ethanols; (RCN)-C-2 nitriles; 2; 2-(R-1)(2)-4-R-2-1; 2-dihydrobenzo[f]isoquinolinium chlorides; analgesic effect; hot-plate test; preventing death from camphor convulsions;
D O I：
10.1007/s11094-020-02113-1
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Ritter cyclocondensation of 2-(1-naphthyl)-1,1-(R-1)(2)-ethanols [R-1 = Me, 2R(1) = (CH2)(4)] with nitriles of general formula R2CN (acetonitrile, benzonitriles, benzyl cyanide, cyanoacetamides) and subsequent treatment of the obtained bases with HCl synthesized a series 2,2-(R-1)(2)-4-R-2-1,2-dihydrobenzo[f]isoquinolinium chlorides. All 10 compounds showed analgesic (antinociceptive) activity in the hot-plate test, exceeding the defensive reflex time of metamizole sodium by 1.7 - 2.5 times. Also, they all exhibited anticonvulsant activity and prevented death from camphor-induced convulsions (28.6 - 100%).
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收藏
页码：1005 / 1008
页数：4
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