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Tackling Microbial Resistance with Isatin-Decorated Thiazole Derivatives: Design, Synthesis, and in vitro Evaluation of Antimicrobial and Antibiofilm Activity
Drug Design, Development and Therapy ( IF 4.8 ) Pub Date : 2022-08-25 , DOI: 10.2147/dddt.s365909 Refaie M Kassab 1 , Sami A Al-Hussain 2 , Nooran S Elleboudy 3 , Amgad Albohy 4 , Magdi E A Zaki 2 , Khaled A M Abouzid 5, 6 , Zeinab A Muhammad 7
Drug Design, Development and Therapy ( IF 4.8 ) Pub Date : 2022-08-25 , DOI: 10.2147/dddt.s365909 Refaie M Kassab 1 , Sami A Al-Hussain 2 , Nooran S Elleboudy 3 , Amgad Albohy 4 , Magdi E A Zaki 2 , Khaled A M Abouzid 5, 6 , Zeinab A Muhammad 7
Affiliation
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.
Keywords: 5-bromoisatin, thiosemicarbazone, hydrazonoyl chlorides, thiazoles, Tyrosyl-tRNA synthetases (TyrRS) inhibitors, antimicrobial, molecular docking, MRSA, antibiofilm
中文翻译：
用靛红修饰的噻唑衍生物解决微生物耐药性：抗菌和抗菌膜活性的设计、合成和体外评价
简介：抗生素耐药性是一个全球性威胁，最近一直在增加，尤其是在抗生素过度使用和滥用的情况下。寻找新的抗生素变得越来越不可或缺。
方法：设计和合成靛红衍生物作为 SB-239629（一种细菌酪氨酸-tRNA 合成酶 (TyrRS) 抑制剂）的替代物。筛选新合成的化合物的抗菌和抗生物膜活性。对接研究用于研究这些化合物与 TyrRS 的潜在结合模式。
结果与讨论：新合成的靛红修饰噻唑衍生物（7b、7d 和 14b）对大肠杆菌显示出有效的抗菌活性，革兰氏阴性菌的代表。此外，7f 显示出对耐甲氧西林金黄色葡萄球菌(MRSA)的最佳活性。此外，发现 7h 和 11f 对白色念珠菌具有与参考制霉菌素相当的抗真菌活性。发现所有具有抗微生物活性的新靛红衍生物在其最低抑菌浓度 (MIC) 的一半时表现出强烈的生物膜扭曲效应。此外，噻唑衍生物 11a-f 显示出有希望的生物膜形成抑制作用。最后，分子对接研究用于研究目标化合物与金黄色葡萄球菌和大肠杆菌TyrRS 的可能结合模式。
结论：新型靛红修饰的噻唑衍生物显示出强大的抗菌和抗真菌活性，对 TyrRS 具有潜在作用。
关键词： 5-溴靛红，氨基硫脲，腙酰氯，噻唑类，酪氨酰-tRNA合成酶（TyrRS）抑制剂，抗菌剂，分子对接，MRSA，抗生物膜
更新日期：2022-08-25
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.
Keywords: 5-bromoisatin, thiosemicarbazone, hydrazonoyl chlorides, thiazoles, Tyrosyl-tRNA synthetases (TyrRS) inhibitors, antimicrobial, molecular docking, MRSA, antibiofilm
中文翻译：
用靛红修饰的噻唑衍生物解决微生物耐药性：抗菌和抗菌膜活性的设计、合成和体外评价
简介：抗生素耐药性是一个全球性威胁，最近一直在增加，尤其是在抗生素过度使用和滥用的情况下。寻找新的抗生素变得越来越不可或缺。
方法：设计和合成靛红衍生物作为 SB-239629（一种细菌酪氨酸-tRNA 合成酶 (TyrRS) 抑制剂）的替代物。筛选新合成的化合物的抗菌和抗生物膜活性。对接研究用于研究这些化合物与 TyrRS 的潜在结合模式。
结果与讨论：新合成的靛红修饰噻唑衍生物（7b、7d 和 14b）对大肠杆菌显示出有效的抗菌活性，革兰氏阴性菌的代表。此外，7f 显示出对耐甲氧西林金黄色葡萄球菌(MRSA)的最佳活性。此外，发现 7h 和 11f 对白色念珠菌具有与参考制霉菌素相当的抗真菌活性。发现所有具有抗微生物活性的新靛红衍生物在其最低抑菌浓度 (MIC) 的一半时表现出强烈的生物膜扭曲效应。此外，噻唑衍生物 11a-f 显示出有希望的生物膜形成抑制作用。最后，分子对接研究用于研究目标化合物与金黄色葡萄球菌和大肠杆菌TyrRS 的可能结合模式。
结论：新型靛红修饰的噻唑衍生物显示出强大的抗菌和抗真菌活性，对 TyrRS 具有潜在作用。
关键词： 5-溴靛红，氨基硫脲，腙酰氯，噻唑类，酪氨酰-tRNA合成酶（TyrRS）抑制剂，抗菌剂，分子对接，MRSA，抗生物膜
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