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N-{[(6-取代-1,3-苯并噻唑-2-基)氨基]硫代甲酰基}-2/4-取代苯甲酰胺:合成与药理评价

N-{[(6-substituted-1,3-benzothiazole-2-yl)amino]carbonothioyl}-2/4-substituted benzamides: synthesis and pharmacological evaluation.

作者信息

Rana Arpana, Siddiqui Nadeem, Khan Suroor A, Ehtaishamul Haque Syed, Bhat Mashooq A

机构信息

Hamdard University, Faculty of Pharmacy, Department of Pharmaceutical Chemistry, New Delhi 110 062, India.

出版信息

Eur J Med Chem. 2008 May;43(5):1114-22. doi: 10.1016/j.ejmech.2007.07.008. Epub 2007 Jul 29.

DOI:10.1016/j.ejmech.2007.07.008
PMID:17826870
Abstract

A series of 1,3-benzothiazol-2-yl benzamides (11-30) were prepared in satisfactory yield and evaluated for their anticonvulsant, neurotoxicity, CNS depressant study and other toxicity studies. All the synthesized compounds were in good agreement with elemental and spectral data. Majority of the compounds were active in MES and scPTZ screen and showed the decrease in the immobility time. None of the compounds had shown neurotoxicity or liver toxicity.

摘要

制备了一系列1,3 - 苯并噻唑 - 2 - 基苯甲酰胺(11 - 30),产率令人满意,并对其进行了抗惊厥、神经毒性、中枢神经系统抑制研究及其他毒性研究。所有合成的化合物与元素分析和光谱数据吻合良好。大多数化合物在最大电休克(MES)和皮下注射戊四氮(scPTZ)筛选中具有活性,并显示出不动时间减少。没有一种化合物表现出神经毒性或肝毒性。

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