7-(2-(2-(3-(取代苯基)丙烯酰)苯氧基)乙氧基)-4-甲基- 2h - chromen -2 - ones的合成、计算及药理评价

Sushil Kumar, Amit Kumar
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引用次数: 0

摘要

背景:受杂交分子在医学和治疗方面令人兴奋的生物学潜力的驱使。利用化学杂交技术研究香豆素-查尔酮对骨骼肌和抗焦虑的作用。目的:由于其众多的优点,包括高效、对受体的作用方式、最小的副作用和改进的药代动力学特征,自然发生和合成的杂化化合物是新型药物开发技术的潜在来源。鉴于这些应用,我们设计了一些香豆素-查尔酮复合物,并探索了它们在骨骼肌和抗焦虑方面的潜力。方法:采用化学杂交方法合成香豆素-查尔酮复合物,并对其骨骼肌和抗焦虑活性进行评价。目标化合物由7-羟基-4-甲基coumarion与卤代烷烃反应得到7-(2-溴乙氧基)-4-甲基- 2h - chromen2 -one,再用羟基查尔酮处理。目的化合物的结构通过熔点、薄层色谱、红外、核磁共振和质量研究得到了证实。目标化合物的计算性质也通过在线软件确定。对瑞士白化病小鼠进行骨骼肌和抗焦虑电位测定。结果:香豆素-查尔酮复合物在瑞士白化病小鼠中显示出骨骼肌和抗焦虑的潜力,与地西泮相比,目标化合物的计算特性也显示出相似。结论:在靶化合物中,含氟基团的化合物比标准药物地西泮更有效。
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Synthesis, Computational and Pharmacological Evaluation of 7-(2-(2- (3- (Substituted Phenyl) Acryloyl) Phenoxy) Ethoxy)-4-Methyl-2H-Chromen- 2-Ones as CNS Agents.

Background: Motivated by the exciting biological potential for the use of hybrid molecules in medicine and therapy. It is anticipated that the coumarin-chalcone hybrids for skeletal muscle and antianxiety action will be investigated using a chemical hybridization technique.

Objective: Due to its numerous benefits, including high effectiveness, mode of action at receptors, minimal adverse effects, and improved pharmacokinetic features, naturally occurring and synthesized hybrid compounds are prospective sources for novel drug development techniques. In opinion of these applications, we here designed some coumarin-chalcone hybrids and explored them for skeletal muscle and antianxiety potential.

Methods: Using a chemical hybridization strategy, coumarin-chalcone hybrids have been synthesized and evaluated for skeletal muscle and antianxiety activity. The target compounds were synthesized by reaction of 7-hydroxy-4-methylcoumarion with haloalkane to afford 7-(2- bromoethoxy)-4-methyl-2H-chromen-2-one which was further treated with hydroxychalcones. The structures of target compounds were confirmed on the basis of their Melting Point, Thin Layer Chromatography, IR, 1HNMR and Mass studies. The computational properties of target compounds were also determined through online software. Skeletal muscle and antianxiety potential were performed in Swiss albino mice.

Results: The coumarin-chalcones hybrids showed skeletal muscle and antianxiety potential in Swiss albino mice and computational properties of the target compounds were also showed similarity as compared with diazepam.

Conclusion: Among the target compounds, the fluoro group containing compound was found to be more potent as compared to the standard drug diazepam.

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来源期刊
Central nervous system agents in medicinal chemistry
Central nervous system agents in medicinal chemistry Psychology-Neuropsychology and Physiological Psychology
CiteScore
2.10
自引率
0.00%
发文量
21
期刊介绍: Central Nervous System Agents in Medicinal Chemistry aims to cover all the latest and outstanding developments in medicinal chemistry and rational drug design for the discovery of new central nervous system agents. Containing a series of timely in-depth reviews written by leaders in the field covering a range of current topics, Central Nervous System Agents in Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments in the field.
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