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Design, synthesis, antimicrobial, and DNA gyrase inhibitory properties of fluoroquinolone-dichloroacetic acid hybrids.
Chemical Biology & Drug Design ( IF 3.2 ) Pub Date : 2019-11-02 , DOI: 10.1111/cbdd.13638 Israa A Seliem 1, 2 , Siva S Panda 1 , Adel S Girgis 3 , Yosra I Nagy 4 , Riham F George 5 , Walid Fayad 6 , Nehmedo G Fawzy 3 , Tarek S Ibrahim 2, 7 , Amany M M Al-Mahmoudy 2 , Rajeev Sakhuja 8 , Zakaria K M Abdel-Samii 2
Chemical Biology & Drug Design ( IF 3.2 ) Pub Date : 2019-11-02 , DOI: 10.1111/cbdd.13638 Israa A Seliem 1, 2 , Siva S Panda 1 , Adel S Girgis 3 , Yosra I Nagy 4 , Riham F George 5 , Walid Fayad 6 , Nehmedo G Fawzy 3 , Tarek S Ibrahim 2, 7 , Amany M M Al-Mahmoudy 2 , Rajeev Sakhuja 8 , Zakaria K M Abdel-Samii 2
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A series of new fluoroquinolone conjugates 8a-g and 9a-f were synthesized via benzotriazole-mediated synthetic approach with good yield and purity. Some of the synthesized analogs exhibited significant antibacterial properties against Escherichia coli and Staphylococcus aureus with potency higher than that of the parent drugs through in vitro standard bioassay procedure (conjugates 8c and 8d reveal antimicrobial properties with potency 1.9, 61.9, 20.7 and 2.4, 37.1, 8.3 folds relative to the parent antibiotic 6 against E. coli, S. aureus, and Enterococcus faecalis, respectively). The observed experimental data were supported by enzymatic DNA gyrase inhibitory property. Developed BMLR-QSAR model validates the observed experimental data and recognizes the parameters responsible for the enhanced antibacterial properties.
中文翻译：
氟喹诺酮-二氯乙酸杂化物的设计，合成，抗菌和DNA促旋酶抑制特性。
通过苯并三唑介导的合成方法合成了一系列新的氟喹诺酮共轭物8a-g和9a-f，并具有良好的收率和纯度。通过体外标准生物测定方法，一些合成的类似物对大肠杆菌和金黄色葡萄球菌显示出显着的抗菌性能，其效力高于母体药物（结合物8c和8d的抗菌性能分别为1.9、61.9、20.7和2.4、37.1，相对于母体抗生素6分别抗大肠杆菌，金黄色葡萄球菌和粪肠球菌的8.3倍。观察到的实验数据得到酶促DNA促旋酶抑制特性的支持。所开发的BMLR-QSAR模型验证了观察到的实验数据并识别了增强抗菌性能的参数。
更新日期：2019-11-04
中文翻译：
氟喹诺酮-二氯乙酸杂化物的设计，合成，抗菌和DNA促旋酶抑制特性。
通过苯并三唑介导的合成方法合成了一系列新的氟喹诺酮共轭物8a-g和9a-f，并具有良好的收率和纯度。通过体外标准生物测定方法，一些合成的类似物对大肠杆菌和金黄色葡萄球菌显示出显着的抗菌性能，其效力高于母体药物（结合物8c和8d的抗菌性能分别为1.9、61.9、20.7和2.4、37.1，相对于母体抗生素6分别抗大肠杆菌，金黄色葡萄球菌和粪肠球菌的8.3倍。观察到的实验数据得到酶促DNA促旋酶抑制特性的支持。所开发的BMLR-QSAR模型验证了观察到的实验数据并识别了增强抗菌性能的参数。
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