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Arylidene and amino spacer-linked rhodanine-quinoline hybrids as upgraded antimicrobial agents
Chemical Biology & Drug Design ( IF 3.2 ) Pub Date : 2023-09-12 , DOI: 10.1111/cbdd.14345 Zebabanu Khalifa 1 , Rachana Upadhyay 1 , Amit B. Patel 1
Chemical Biology & Drug Design ( IF 3.2 ) Pub Date : 2023-09-12 , DOI: 10.1111/cbdd.14345 Zebabanu Khalifa 1 , Rachana Upadhyay 1 , Amit B. Patel 1
Affiliation
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Antibiotic resistance associated with various microorganisms such as Gram-positive, Gram-negative, fungal strains, and multidrug-resistant tuberculosis increases the risk of healthcare survival. Preliminary therapeutics becoming ineffective that might lead to noteworthy mortality presents a crucial challenge for the scientific community. Hence, there is an urgent need to develop hybrid compounds as antimicrobial agents by combining two or more bioactive heterocyclic moieties into a single molecular framework with fewer side effects and a unique mode of action. This review highlights the recent advances (2013–2023) in the pharmacology of rhodanine-linked quinoline hybrids as more effective antimicrobial agents. In the drug development process, linker hybrids acquire the top position due to their excellent π-stacking and Van der Waals interaction with the DNA active sites of pathogens. A molecular hybridization strategy has been optimized, indicating that combining these two bioactive moieties with an arylidene and an amino spacer linker increases the antimicrobial potential and reduces drug resistance. Moreover, the structure–activity relationship study is discussed to express the role of various functional groups in improving and decrementing antimicrobial activities for rational drug design. Also, a linker approach may accelerate the development of dynamic antimicrobial agents through molecular hybridization.
中文翻译：
亚芳基和氨基间隔基连接的罗丹宁-喹啉杂化物作为升级的抗菌剂
与各种微生物（例如革兰氏阳性菌、革兰氏阴性菌、真菌菌株和耐多药结核病）相关的抗生素耐药性增加了医疗保健生存的风险。初步治疗无效可能导致显着的死亡率，这对科学界来说是一个严峻的挑战。因此，迫切需要通过将两个或多个生物活性杂环部分组合成具有更少副作用和独特作用模式的单一分子框架来开发作为抗菌剂的混合化合物。本综述重点介绍了绕丹宁连接的喹啉杂化物作为更有效的抗菌剂的药理学最新进展（2013-2023）。在药物开发过程中，连接杂合体因其优异的π堆积和与病原体DNA活性位点的范德华相互作用而占据首位。分子杂交策略已得到优化，表明将这两个生物活性部分与亚芳基和氨基间隔连接基结合可增加抗菌潜力并降低耐药性。此外，还讨论了结构-活性关系研究，以表达各种官能团在提高和降低抗菌活性以实现合理药物设计中的作用。此外，连接子方法可以通过分子杂交加速动态抗菌剂的开发。
更新日期：2023-09-12
中文翻译：
亚芳基和氨基间隔基连接的罗丹宁-喹啉杂化物作为升级的抗菌剂
与各种微生物（例如革兰氏阳性菌、革兰氏阴性菌、真菌菌株和耐多药结核病）相关的抗生素耐药性增加了医疗保健生存的风险。初步治疗无效可能导致显着的死亡率，这对科学界来说是一个严峻的挑战。因此，迫切需要通过将两个或多个生物活性杂环部分组合成具有更少副作用和独特作用模式的单一分子框架来开发作为抗菌剂的混合化合物。本综述重点介绍了绕丹宁连接的喹啉杂化物作为更有效的抗菌剂的药理学最新进展（2013-2023）。在药物开发过程中，连接杂合体因其优异的π堆积和与病原体DNA活性位点的范德华相互作用而占据首位。分子杂交策略已得到优化，表明将这两个生物活性部分与亚芳基和氨基间隔连接基结合可增加抗菌潜力并降低耐药性。此外，还讨论了结构-活性关系研究，以表达各种官能团在提高和降低抗菌活性以实现合理药物设计中的作用。此外，连接子方法可以通过分子杂交加速动态抗菌剂的开发。
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