Deep Aakash, Narasimhan Balasubramanian, Aggarwal Swati, Kaushik Dhirender, Sharma Arun K
Department of Pharmaceutical Sciences, Chaudhary Bansi Lal University, Bhiwani-127021, India.
Cent Nerv Syst Agents Med Chem. 2016;16(2):158-64. doi: 10.2174/1871524916666160204114424.
Heterocyclic compounds are extensively dispersed in nature and are vital for life. Various investigational approaches towards Structural Activity Relationship that focus upon the exploration of optimized candidates have become vastly important.
Literature studies tell that for a series of compounds that are imperative in industrial and medicinal chemistry, thiophene acts as parent. Among various classes of heterocyclic compounds that have potential central nervous system activity, thiophene is the most important one. In the largely escalating chemical world of heterocyclic compounds showing potential pharmacological character, thiophene nucleus has been recognized as the budding entity.
Seventeen Papers were included in this review article to define the central nervous system potential of thiophene. This review article enlightens the rationalized use and scope of thiophene scaffold as novel central nervous system activity such as anticonvulsant, acetylcholinesterase inhibitor, cyclin-dependent kinase 5 (cdk5/p25) inhibitors, CNS depressant, capability to block norepinephrine, serotonin and dopamine reuptake by their respective transporters etc.
The Finding of this review confirm the importance of thiophene scaffold as potential central nervous system agents. From this outcome, ideas for future molecular modifications leading to the novel derivatives with better constructive pharmacological potential may be derived.
杂环化合物广泛分布于自然界,对生命至关重要。各种聚焦于探索优化候选物的构效关系研究方法变得极为重要。
文献研究表明,对于工业和药物化学中一系列至关重要的化合物,噻吩作为母体。在具有潜在中枢神经系统活性的各类杂环化合物中,噻吩是最重要的一种。在显示出潜在药理特性的杂环化合物不断发展的化学领域中,噻吩核已被视为新兴实体。
本综述文章纳入了17篇论文来界定噻吩的中枢神经系统潜力。这篇综述文章阐明了噻吩支架作为新型中枢神经系统活性物质的合理用途和范围,如抗惊厥、乙酰胆碱酯酶抑制剂、细胞周期蛋白依赖性激酶5(cdk5/p25)抑制剂、中枢神经系统抑制剂、通过各自转运体阻断去甲肾上腺素、5-羟色胺和多巴胺再摄取的能力等。
本综述的研究结果证实了噻吩支架作为潜在中枢神经系统药物的重要性。基于这一结果,或许可以得出未来分子修饰的思路,以产生具有更好建设性药理潜力的新型衍生物。