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| Content Provider | Royal Society of Chemistry (RSC) |
|---|---|
| Author | Alagumuthu, Manikandan Arumugam, Sivakumar Sridhar, P. Reddy, Sabbasani Rajasekhara |
| Copyright Year | 2016 |
| Abstract | The (E)-N′-(substituted-benzylidene)-2-(7-fluoro-2-methoxyquinolin-8-yl)acetohydrazide-hydrazone derivatives reported in this manuscript represent a new series of antibacterial agents, as well as DNA gyrase inhibitors. Efforts were made to synthesize these quinolone-acetohydrazide-hydrazone derivatives (9a–n) in excellent yields. All the target compounds were evaluated for their in vitro antimicrobial activity against Escherichia coli (MTCC 443) and Pseudomonas aeruginosa (MTCC 424), as specimens of Gram-negative bacteria, and Staphylococcus aureus (MTCC 96) and Staphylococcus pyogenes (MTCC 442), as specimens of Gram-positive bacteria. Excellent antibacterial activity was observed for compounds substituted with R = 3,4,5-trimethoxy, 4-F, 4-OCF3, 4-CF3, and 3-CF3 moieties. Derivatives 9a–n were docked into the active sites of DNA gyrase A and DNA gyrase B in order to obtain more insight into the binding modes of the compounds. Among all the derivatives, 9n showed the lowest binding energy of −91.6 kcal mol−1 with DNA gyrase A. A DNA gyrase enzyme inhibition assay favors compounds 9m and 9n, which were substituted with di-fluorine moieties (R = 2,4-difluoro and 3,4-difluoro) in the quinoline scaffold, as the most potent inhibitors of S. aureus DNA gyrase A (9m, IC50 0.14 mg mL−1 and 9n, IC50 0.19 mg mL−1). |
| Starting Page | 64460 |
| Ending Page | 64468 |
| Page Count | 9 |
| File Format | HTM / HTML PDF |
| ISSN | 20462069 |
| Volume Number | 6 |
| Issue Number | 69 |
| Journal | RSC Advances |
| DOI | 10.1039/c6ra09891f |
| Language | English |
| Publisher | Royal Society of Chemistry |
| Access Restriction | Open |
| Subject Keyword | Antimicrobial Escherichia coli Gram-positive bacteria Enzyme inhibitor Selective Service System DNA gyrase Aureus Binding energy IC50 Quinoline Pseudomonas aeruginosa Bacteria Gram-negative bacteria |
| Content Type | Text |
| Resource Type | Article |
| Subject | Chemistry Chemical Engineering |
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