Synthesis and Pharmacological Evaluation of Novel Triazolo [4, 3-a] tetrahydrobenzo (b) thieno [3, 2-e] pyrimidine-5(4H)-ones

被引：3

作者：

Thore, S. N. ^{[1
]}

Gupta, Sunil V. ^{[1
]}

Baheti, Kamalkishor G. ^{[2
]}

机构：

[1] Deogiri Coll, Aurangabad 431005, Maharashtra, India

[2] Charak Coll Pharm & Res, Pune 412207, Maharashtra, India

来源：

JOURNAL OF HETEROCYCLIC CHEMISTRY | 2015年 / 52卷 / 01期

关键词：

SUBSTITUTED 1,3,4-OXADIAZOLE DERIVATIVES; AROMATIC CARBOXYLIC-ACID; ONE-POT; BENZODIAZEPINE RECEPTORS; 4-COMPONENT SYNTHESIS; ANXIOLYTIC ACTIVITY; DEPRESSANT ACTIVITY; ANXIETY; SERIES; AMINE;

D O I：

10.1002/jhet.1989

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

Triazolo[4,3-a]tetrahydrobenzo(b)thieno[3,2-e]pyrimidine-5(4H)-ones (5a, 5b, 5c, 5d, 5e, 5f, 5g, 5h, 5i, 5j, 5k, 5l, 5m were synthesized and characterized by spectral analysis. All 13 derivatives were evaluated for central nervous system (CNS) depressant and skeletal muscle relaxant activities in Swiss albino mice. All the activities were compared with diazepam as a standard drug at a dose of 5mg/kg. The most active derivatives 5d, 5e, 5k, and 5l in CNS depressant and skeletal muscle relaxant activities were selected for anticonvulsant activity. The active derivatives were found to protect 100% mice at the dose of 6-11mg/kg, where as standard diazepam protect the animal at a dose of 2.5mg/kg.

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页码：142 / 149

页数：8

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