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Morpholine as ubiquitous pharmacophore in medicinal chemistry: Deep insight into the structure-activity relationship (SAR).
Bioorganic Chemistry ( IF 4.5 ) Pub Date : 2020-01-11 , DOI: 10.1016/j.bioorg.2020.103578
Archana Kumari 1 , Rajesh K Singh 2
Affiliation  

Morpholine is a versatile moiety, a privileged pharmacophore and an outstanding heterocyclic motif with wide ranges of pharmacological activities due to different mechanisms of action. The ability of morpholine to enhance the potency of the molecule through molecular interactions with the target protein (kinases) or to modulate the pharmacokinetic properties propelled medicinal chemists and researchers to synthesize morpholine ring by the efficient ways and to incorporate this moiety to develop various lead compounds with diverse therapeutic activities. The present review primarily focused on discussing the most promising synthetic leads containing morpholine ring along with structure-activity relationship (SAR) to reveal the active pharmacophores accountable for anticancer, anti-inflammatory, antiviral, anticonvulsant, antihyperlipidemic, antioxidant, antimicrobial and antileishmanial activity. This review outlines some of the recent effective chemical synthesis for morpholine ring. The review also highlighted the metabolic liability of some clinical drugs containing this nucleus and various researches on modified morpholine to enhance the metabolic stability of drugs as well. Drugs bearing morpholine ring and those under clinical trials are also mentioned with the role of morpholine and their mechanism of action. This review will provide the necessary knowledge base to the medicinal chemists in making strategic structural changes in designing morpholine derivatives.

中文翻译:

吗啉作为药物化学中普遍存在的药效团:深入了解结构-活性关系(SAR)。

吗啉是一种多用途的部分,一种特权的药效基团和一种杰出的杂环基序,由于不同的作用机理而具有广泛的药理活性。吗啉通过与靶蛋白(激酶)的分子相互作用来增强分子效力或调节药代动力学特性的能力推动了药物化学家和研究人员通过有效方式合成吗啉环并结合该部分以开发各种先导化合物具有多种治疗作用。目前的审查主要集中于讨论最有希望的包含吗啉环的合成前导以及结构-活性关系(SAR),以揭示负责抗癌,抗炎,抗病毒,抗惊厥,降血脂,抗氧化剂,抗菌剂和抗菌剂活性。这篇综述概述了吗啉环的一些最近有效的化学合成方法。综述还强调了一些含有该核的临床药物的代谢作用,以及对修饰吗啉以增强药物代谢稳定性的各种研究。还提到了带有吗啉环的药物以及正在临床试验中的药物,它们具有吗啉的作用及其作用机理。这篇综述将为药物化学家在设计吗啉衍生物进行战略结构变化时提供必要的知识基础。综述还强调了一些含有该核的临床药物的代谢作用,以及对修饰吗啉以增强药物代谢稳定性的各种研究。还提到了带有吗啉环的药物以及正在临床试验中的药物,它们具有吗啉的作用及其作用机理。这篇综述将为药物化学家在设计吗啉衍生物进行战略结构变化时提供必要的知识基础。综述还强调了一些含有该核的临床药物的代谢责任,以及对修饰吗啉以增强药物代谢稳定性的各种研究。还提到了带有吗啉环的药物以及正在临床试验中的药物,它们具有吗啉的作用及其作用机理。这篇综述将为药物化学家在设计吗啉衍生物进行战略结构变化时提供必要的知识基础。
更新日期:2020-01-13
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