微波辅助下苯并咪唑衍生物的绿色合成及其抗惊厥活性评价

IF 0.9 Q4 CHEMISTRY, MULTIDISCIPLINARY Current Microwave Chemistry Pub Date : 2019-10-24 DOI:10.2174/2213335606666190429124745
B. Sahoo, B. Banik, Mazaharunnisa, N. Rao, B. Raju
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引用次数: 15

摘要

苯并咪唑是稠合杂环芳香族化合物。它是开发新药分子所必需的α-armacophore和特权结构。这些是存在于各种驱虫药物中的生物活性分子,如阿苯达唑、甲苯达唑、对苯达唑和三氯苯达唑等。苯并咪唑衍生物是由邻苯二胺和邻苯二甲酸反应,然后在醋酸酐存在下乙酰化合成的。最后,乙酰化产物与各种取代的苯甲醛进行克莱森-席姆德缩合,产生具有生态反应的苯并咪唑衍生物或查尔酮。采用常规和微波辐照技术制备了标题化合物。筛选了标题化合物的抗惊厥和神经毒性活性。通过微波合成,在较短的反应时间内提高了产物的产率。因此,它遵循绿色化学的方法,使上述反应环保。与标准药物相比,一些化合物具有显著的抗惊厥活性。在本研究中,我们合成了具有查尔酮部分的新型苯并咪唑衍生物,以提高其生物活性。这些化合物是在微波反应下在短反应时间内以高产率获得的。
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Microwave Assisted Green Synthesis of Benzimidazole Derivatives and Evaluation of Their Anticonvulsant Activity
Benzimidazole is the fused heterocyclic aromatic compound. It is an essential pharmacophore and privileged structure for the development of new drug molecules. These are bioactive molecules present in various anthelmintic drugs such as albendazole, mebendazole, parbendazole, triclabendazole etc. Benzimidazole derivatives are synthesized by reaction between orthophenylene diamine and anthranillic acid followed by acetylation in the presence of acetic anhydride. Finally, the acetylated products undergo Claisen-Schimdt condensation with various substituted benzaldehydes to produce corresponding benzimidazole derivatives or chalcones. Both conventional and microwave irradiation technology are followed to get the titled compounds. The titled compounds are screened for their anticonvulsant and neurotoxicity activity. By the help of microwave synthesis, the yield of product was increased in less reaction time. So, it follows Green chemistry approach by making above reactions eco-friendly. Some of the compounds exhibited significant anticonvulsant activity as compared to standard drug. In the present investigation, we have synthesized novel benzimdazole derivatives with chalone moiety to improve the biological activity. The compounds were obtained under microwave reaction with high yield in a short reaction time.
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来源期刊
Current Microwave Chemistry
Current Microwave Chemistry CHEMISTRY, MULTIDISCIPLINARY-
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