4.7 Article

Tackling Microbial Resistance with Isatin-Decorated Thiazole Derivatives: Design, Synthesis, and in vitro Evaluation of Antimicrobial and Antibiofilm Activity

期刊

DRUG DESIGN DEVELOPMENT AND THERAPY
卷 16, 期 -, 页码 2817-2832

出版社

DOVE MEDICAL PRESS LTD
DOI: 10.2147/DDDT.S365909

关键词

5-bromoisatin; thiosemicarbazone; hydrazonoyl chlorides; thiazoles; Tyrosyl-tRNA synthetases (TyrRS) inhibitors; antimicrobial; molecular docking; MRSA; antibiofilm

资金

  1. deanship of scientific research, Imam Mohammad Ibn Saud Islamic University, Saudi Arabia [RG-21-09-77]

向作者/读者索取更多资源

This study designed and synthesized novel isatin-decorated thiazole derivatives that exhibited strong antimicrobial and antifungal activities, potentially targeting TyrRS. These compounds showed antimicrobial activity against gram-negative bacteria and Methicillin Resistant Staphylococcus aureus (MRSA), as well as antifungal activity against Candida albicans and biofilm formation inhibition.
Introduction: Antibiotic resistance is a global threat that has been increasing recently, especially with antibiotic overuse and misuse. The search for new antibiotics is becoming more and more indispensable.Methods: Design and synthesis of isatin derivatives as surrogates of SB-239629, a bacterial tyrosine-tRNA synthetases (TyrRS) inhibitor. The newly synthesized compounds were screened for their antimicrobial and antibiofilm activities. Docking studies were used to investigate potential binding modes of these compounds with TyrRS. Results and Discussion: Newly synthesized isatin-decorated thiazole derivatives (7b, 7d, and 14b) have shown potent antimicrobial activities against E. coli, a representative of gram-negative bacteria. Also, 7f showed the best activity against Methicillin Resistant Staphylococcus aureus (MRSA). In addition, 7h and 11f were found to have antifungal activities against Candida albicans equivalent to that of the reference Nystatin. All the new isatin derivatives with antimicrobial activities were found to exhibit strong biofilm distortion effects at half their minimum inhibitory concentrations (MIC). Moreover, thiazole derivatives 11a-f showed promising biofilm formation inhibition. Finally, molecular docking studies were used to investigate possible binding modes of target compounds with S. aureus and E. coli TyrRS.Conclusion: The novel isatin-decorated thiazole derivatives show strong antimicrobial and antifungal activities with potential action on TyrRS.

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