Cheke Rameshwar S, Patel Harun M, Patil Vaishali M, Ansari Iqrar Ahmad, Ambhore Jaya P, Shinde Sachin D, Kadri Adel, Snoussi Mejdi, Adnan Mohd, Kharkar Prashant S, Pasupuleti Visweswara Rao, Deshmukh Prashant K
Department of Pharmaceutical Chemistry, Dr. Rajendra Gode College of Pharmacy, Malkapur 443101, India.
Department of Pharmaceutical Chemistry, R. C. Patel Institute of Pharmaceutical Education and Research, Shirpur 425405, India.
Antibiotics (Basel). 2022 Apr 24;11(5):566. doi: 10.3390/antibiotics11050566.
A major global health risk has been witnessed with the development of drug-resistant bacteria and multidrug-resistant pathogens linked to significant mortality. Coumarins are heterocyclic compounds belonging to the benzophenone class enriched in different plants. Coumarins and their derivatives have a wide range of biological activity, including antibacterial, anticoagulant, antioxidant, anti-inflammatory, antiviral, antitumour, and enzyme inhibitory effects. In the past few years, attempts have been reported towards the optimization, synthesis, and evaluation of novel coumarin analogues as antimicrobial agents. Several coumarin-based antibiotic hybrids have been developed, and the majority of them were reported to exhibit potential antibacterial effects. In the present work, studies reported from 2016 to 2020 about antimicrobial coumarin analogues are the focus. The diverse biological spectrum of coumarins can be attributed to their free radical scavenging abilities. In addition to various synthetic strategies developed, some of the structural features include a heterocyclic ring with electron-withdrawing/donating groups conjugated with the coumarin nucleus. The suggested structure-activity relationship (SAR) can provide insight into how coumarin hybrids can be rationally improved against multidrug-resistant bacteria. The present work demonstrates molecular insights for coumarin derivatives having antimicrobial properties from the recent past. The detailed SAR outcomes will benefit towards leading optimization during the discovery and development of novel antimicrobial therapeutics.
随着耐药细菌和与高死亡率相关的多重耐药病原体的出现，一种重大的全球健康风险已被见证。香豆素是属于二苯甲酮类的杂环化合物，在不同植物中含量丰富。香豆素及其衍生物具有广泛的生物活性，包括抗菌、抗凝、抗氧化、抗炎、抗病毒、抗肿瘤和酶抑制作用。在过去几年中，已有报道尝试对新型香豆素类似物进行优化、合成和评估，以作为抗菌剂。已经开发了几种基于香豆素的抗生素杂化物，据报道其中大多数具有潜在的抗菌作用。在本工作中，重点是2016年至2020年报道的关于抗菌香豆素类似物的研究。香豆素多样的生物谱可归因于其自由基清除能力。除了开发的各种合成策略外，一些结构特征包括带有与香豆素核共轭的吸电子/供电子基团的杂环。建议的构效关系（SAR）可以深入了解如何合理改进香豆素杂化物以对抗多重耐药细菌。本工作展示了近期具有抗菌特性的香豆素衍生物的分子见解。详细的SAR结果将有助于在新型抗菌疗法的发现和开发过程中进行领先优化。
