Synthesis of benzothiazole derivatives having acetamido and carbothioamido pharmacophore as anticonvulsant agents

被引：35

作者：

Amir, Mohd. ^{[1
]}

Asif, S. ^{[1
]}

Ali, Israr ^{[1
]}

Hassan, Mohd Zaheen ^{[1
]}

机构：

[1] Hamdard Univ, Dept Pharmaceut Chem, Fac Pharm, New Delhi 110062, India

来源：

MEDICINAL CHEMISTRY RESEARCH | 2012年 / 21卷 / 09期

关键词：

Benzothiazole; Acetamide; Carbothioamide; Drug-likeness; Anticonvulsant activity; DESIGN; SEMICARBAZONES; DISCOVERY; EPILEPSY; DRUGS; RATS;

D O I：

10.1007/s00044-011-9791-1

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A new series of N-(6-chlorobenzothiazol-2-yl)-2-substituted-acetamides (3a-h) and N-(6-chlorobenzothiazol-2-yl)-2-(substituted-benzylidene)hydrazinecarbothioamides (5a-h) were synthesized and characterized by IR, H-1 NMR, mass and elemental analysis. In vivo anticonvulsant and acute toxicity screening of all the synthesized compounds showed morpholino (3f) and imidazolyl (3g) derivatives as promising anticonvulsant lead. Furthermore, In silico drug-likeness parameters have also been investigated for filtering out the likelihood of poor drug absorption or brain penetration. 3D four-point pharmacophore measurements of compounds were also carried out to match these with established anticonvulsants agents.

引用

页码：2661 / 2670

页数：10