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首页> 外文期刊>Anti-infective agents >Anti-mitotic Activity of the Benzothiazole-pyrazole Hybrid Derivatives
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Anti-mitotic Activity of the Benzothiazole-pyrazole Hybrid Derivatives

机译：苯并噻唑 - 吡唑杂交衍生物的抗丝分裂活性

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Background: Nitrogen-containing heterocyclics are abundant in natural products andalso in synthetic drug molecules because of a variety of applications and superior pharmacologicalprofile action. Pyrazoles are the integral architects of many of the heterocyclic compounds with superiorbiological activity.Methods: Two series of the pyrazole conjugated Benzothiazole derivatives were synthesized. Thepyrazoles were synthesized by the Vilsmeier-Haack reaction and then conjugated with benzothiazolehydrazine and hydrazide by imine bond formation. The synthesized compounds were screenedfor anti-mitotic activity using Allium assay.Results: Here, the anti-mitotic activity, the percentage of cell division and the percentage of inhibitioncompared to the control were calculated. Compound 4b (-OMe), 4c (-OH), 5b (-OMe), 5c (-OH) and 5d (-CH3) had electron donating groups which showed excellent activity, was followed by4f and 5f where they contain p-Bromo substitution, showing moderate activity.Conclusion: In the two series, benzothiazole linked to pyrazole through the hydrazide bridging(5a-5i) had superior to hydrazine bridging (4a-4i). The observed chromosomal aberrations are becauseof the structural morphology and binding sites of the molecule with the chromosome.
机译：背景：含氮杂环在合成药物分子中的天然产物中含有丰富的杂环，因为各种应用和优异的药物化学性能。吡唑是许多具有高级学活性的杂环化合物的整体建筑师。方法：合成了两系列吡唑共轭苯并噻唑衍生物。通过Vilsmeier-Haack反应合成了吡唑，然后通过亚胺键形成与苯并噻唑肼和酰肼缀合。使用艾滋病assay筛选合成的化合物。结果：这里，计算抗筛选活动，细胞分裂的百分比和对对照的抑制率的百分比。化合物4b（oom），4℃（-OOH），5b（ - -OH）和5d（-CH3）具有显示出优异的活性的电子捐赠基团，其次是它们含有p-bromo的4F和5f替代，显示适度的活性。结论：在两个系列中，通过酰肼桥接（5a-5i）与吡唑连接的苯并噻唑优于肼桥（4a-4i）。观察到的染色体像差是因为分子与染色体的结构形态和结合位点。

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