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Design and Synthesis of 2-(4-Bromophenyl)Quinoline-4-Carbohydrazide Derivatives via Molecular Hybridization as Novel Microbial DNA-Gyrase Inhibitors.

ABSTRACT: Microbial DNA gyrase is regarded as an outstanding microbial target. Hence, 15 new quinoline derivatives (5-14) were designed and synthesized. The antimicrobial activity of the afforded compounds was pursued via in vitro approaches. The investigated compounds displayed eligible MIC values, particularly against G-positive Staphylococcus aureus species. Consequently, an S. aureus DNA gyrase supercoiling assay was performed, using ciprofloxacin as a reference control. Obviously, compounds 6b and 10 unveiled IC50 values of 33.64 and 8.45 μM, respectively. Alongside, ciprofloxacin exhibited an IC50 value of 3.80 μM. Furthermore, a significant docking binding score was encountered by compound 6b (-7.73 kcal/mol), surpassing ciprofloxacin (-7.29 kcal/mol). Additionally, both compounds 6b and 10 revealed high GIT absorption without passing the blood brain barrier. Finally, the conducted structure-activity relationship study assured the usefulness of the hydrazine moiety as a molecular hybrid for activity either in cyclic or opened form.

SUBMITTER: Abd El-Lateef HM 

PROVIDER: S-EPMC10210181 | biostudies-literature | 2023 May

REPOSITORIES: biostudies-literature

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Design and Synthesis of 2-(4-Bromophenyl)Quinoline-4-Carbohydrazide Derivatives <i>via</i> Molecular Hybridization as Novel Microbial DNA-Gyrase Inhibitors.

Abd El-Lateef Hany M HM   Elmaaty Ayman Abo AA   Abdel Ghany Lina M A LMA   Abdel-Aziz Mohamed S MS   Zaki Islam I   Ryad Noha N  

ACS omega 20230511 20

Microbial DNA gyrase is regarded as an outstanding microbial target. Hence, 15 new quinoline derivatives (<b>5</b>-<b>14</b>) were designed and synthesized. The antimicrobial activity of the afforded compounds was pursued via <i>in vitro</i> approaches. The investigated compounds displayed eligible MIC values, particularly against G-positive <i>Staphylococcus aureus</i> species. Consequently, an <i>S. aureus</i> DNA gyrase supercoiling assay was performed, using ciprofloxacin as a reference cont  ...[more]

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