期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 219, 期 -, 页码 -出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2021.113442
关键词
Oxadiazole; MRSA; SAR; Antibiotics; Drug discovery
资金
- Ph. D Research Startup Foundation of Yulin University Grant [20GK04, 20GK05]
- School of Chemistry and Chemical Engineering, Yulin University
MRSA is becoming a major concern due to its rapid resistance development, prompting the need for novel antibiotics. The oxadiazole moiety serves as an interesting and adaptable molecular structure with potential for research and development as antibacterial agents. Studies on oxadiazole-containing derivatives as potent antibacterial agents against multidrug-resistant MRSA strains and exploring structure-activity relationships have been conducted, providing valuable insights for future drug development.
Methicillin-resistant Staphylococcus aureus (MRSA) is becoming dangerous to human beings due to easy transmission mode and leading to the difficult-to-treat situation. The rapid resistance development of MRSA to many approved antibiotics is of major concern. There is a lot of scope to develop novel, efficient, specific, and nontoxic drug candidates to fight against MRSA isolates. The interesting molecular structure and adaptable feature of oxadiazole moiety which are bioisosteres of esters and amides, and these functional groups show improved resistance to esterases mediated hydrolytic cleavage, attracting researchers to develop required novel antibiotics based on oxadiazole core. This review summarizes the developments of oxadiazole-containing derivatives as potent antibacterial agents against multidrug-resistant MRSA strains and discussing the structure-activity relationship (SAR) in various directions. The current survey is the highlight of the present scenario of oxadiazole hybrids on MRSA studies, covering articles published from 2011 to 2020. This collective information may become a good platform to plan and develop new oxadiazole-based small molecule growth inhibitors of MRSA with minimal side effects. (C) 2021 Elsevier Masson SAS. All rights reserved.
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