Antibacterial activities with the structure-activity relationship of coumarin derivatives

• Published in: European journal of medicinal chemistry Vol. 207; p. 112832
• Main Authors: Qin, Hua-Li, Zhang, Zai-Wei, Ravindar, Lekkala, Rakesh, K.P.
• Format: Journal Article
• Language: English
• Published: France Elsevier Masson SAS 01.12.2020
• Subjects: Anti-Bacterial Agents - chemistry; Anti-Bacterial Agents - pharmacology; Bacteria; Coumarin; Coumarins - chemistry; Coumarins - pharmacology; Drug Resistance, Bacterial - drug effects; Drug Resistance, Multiple - drug effects; Molecular docking; Multidrug-resistance; SAR; Structure-Activity Relationship; Bacteria; SAR; Coumarin; Multidrug-resistance; Molecular docking
• ISSN: 0223-5234; 1768-3254
• DOI: 10.1016/j.ejmech.2020.112832

The development of drug-resistant bacteria, as well as multidrug-resistant pathogens related to substantial mortality, is an important global health threat. The wide range of biological activities and the wealthy use of coumarin-containing drugs in the clinic have encouraged more and more interest in this class of heterocycles. Various coumarin-based antibiotic hybrids have been developed in the last decade and most of them exhibited potential antibacterial potency. This present review summarizes the current innovations of coumarin-based derivatives with potential antibacterial activities against a variety of Gram-negative and Gram-positive bacteria discussing various aspects of structure-activity relationship (SAR). The improved SAR will provide further insight into the rational improvement of coumarin hybrids with astounding strength against multidrug-resistant bacteria. [Display omitted] •Coumarin-based derivatives exhibited potential antibacterial activities.•Detailed explanation of structure-activity relationships (SAR).•EDGs and EWGs play a key role in increasingantibacterial activities.•Rational design and development of coumarin hybrids against multidrug-resistant bacteria.