异恶唑衍生物的绿色化学合成及其抗癫痫活性评价。

Q3 Pharmacology, Toxicology and Pharmaceutics
Krishna Chandra Panda, Ravi Kumar Venkata Varaha Bera, Biswa Mohan Sahoo, Parijat Swain
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引用次数: 0

摘要

背景:绿色战略涉及化学物质的设计、合成、加工和使用,通过消除化学危害的产生。这种方法侧重于原子经济,使用更安全的溶剂或化学品,消耗能源,并将化学物质分解为无毒的环保材料。目的:因此,微波辐照加热法被认为是一种绿色可持续的技术,可用于通过查尔酮类化合物制备新型杂环类支架异恶唑衍生物。异恶唑衍生物具有多种药理活性,如抗生素(磺胺甲恶唑、氯西林、氟氯西林、环丝氨酸)、抗真菌药(德拉唑隆)、抗风湿药(来氟米特)、抗抑郁药(异carboxazid)、抗肿瘤药(Acivicin)、抗惊厥药(唑尼沙胺)、抗精神病药(利培酮)和抗炎药(伐地昔布)等,发挥着至关重要的作用。方法:采用微波辐照法合成异恶唑衍生物,采用绿色化学方法。结果:对标题化合物进行了抗癫痫评价,以确定其治疗潜力。结论:与传统的加热方法相比,微波辐射提高了反应速率,选择性高,产物收率提高。与标准药物(苯妥英)相比,所测试的化合物显示出有希望的抗癫痫活性。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Green Chemistry Approach for the Synthesis of Isoxazole Derivatives and Evaluation of their Anti-epileptic Activity.

Background: Green strategy involves the design, synthesis, processing, and use of chemical substances by eliminating the generation of chemical hazards. This approach focuses on atom economy, use of safer solvents or chemicals, consumption of energy, and decomposition of the chemical substances to non-toxic materials which are eco-friendly.

Objective: So, the microwave irradiated heating method is considered a green and sustainable technique for the development of novel heterocyclic scaffold-like isoxazole derivatives via chalcones. Isoxazole derivatives play a vital role due to their diverse pharmacological activities such as antibiotic (Sulfamethoxazole, Cloxacillin, Flucloxacillin, Cycloserine), anti-fungal (Drazoxolon), Antirheumatic (Leflunomide), antidepressant (Isocarboxazid), antineoplastic (Acivicin), anticonvulsant (Zonisamide), antipsychotic (Risperidone) and anti-inflammatory drugs (Valdecoxib), etc. Methods: The isoxazole derivatives were synthesized with the help of microwave irradiation that follows green chemistry protocol.

Results: The titled compounds were subjected to antiepileptic evaluation to determine their therapeutic potential.

Conclusion: The use of microwave radiation enhances the rate of the reaction which leads to high selectivity with improved product yields in comparison with the traditional heating methods. The tested compounds exhibited promising antiepileptic activity as compared to the standard drug (Phenytoin).

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来源期刊
Current drug discovery technologies
Current drug discovery technologies Pharmacology, Toxicology and Pharmaceutics-Drug Discovery
CiteScore
3.70
自引率
0.00%
发文量
48
期刊介绍: Due to the plethora of new approaches being used in modern drug discovery by the pharmaceutical industry, Current Drug Discovery Technologies has been established to provide comprehensive overviews of all the major modern techniques and technologies used in drug design and discovery. The journal is the forum for publishing both original research papers and reviews describing novel approaches and cutting edge technologies used in all stages of drug discovery. The journal addresses the multidimensional challenges of drug discovery science including integration issues of the drug discovery process.
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