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Most of the target compounds demonstrated good to moderate antimicrobial activity compared with ciprofloxacin and fluconazole. Four compounds (\n                    <jats:bold>8b<\/jats:bold>\n                    ,\n                    <jats:bold>9a<\/jats:bold>\n                    ,\n                    <jats:bold>9c<\/jats:bold>\n                    , and\n                    <jats:bold>10a<\/jats:bold>\n                    ) showed encouraging results, with minimal inhibitory concentration (MIC) values (53.45\u2013258.32\u2009\u00b5M) comparable to those of norfloxacin (100.31\u2013200.63\u2009\u00b5M) and ciprofloxacin (48.33\u201396.68\u2009\u00b5M). Noticeably, the four derivatives revealed excellent bactericidal and fungicidal activities, except for the bacteriostatic potential of compounds\n                    <jats:bold>8b<\/jats:bold>\n                    and\n                    <jats:bold>9a<\/jats:bold>\n                    against\n                    <jats:italic>Escherichia coli<\/jats:italic>\n                    and\n                    <jats:italic>Staphylococcus aureus<\/jats:italic>\n                    , respectively. The time\u2010killing kinetic study against\n                    <jats:italic>S. aureus<\/jats:italic>\n                    confirmed the efficacy of these derivatives. Furthermore, two of the four promising derivatives,\n                    <jats:bold>9a<\/jats:bold>\n                    and\n                    <jats:bold>10a<\/jats:bold>\n                    , could prevent the formation of biofilms of\n                    <jats:italic>S. aureus<\/jats:italic>\n                    without affecting the bacterial growth at low concentrations. A combination study with seven commercial antibiotics against the multidrug\u2010resistant bacterium\n                    <jats:italic>P. aeruginosa<\/jats:italic>\n                    showed a notable reduction in the antibiotic MIC values, represented mainly through a synergistic or additive effect. The enzymatic assay implied that the most active derivatives had inhibition potency against DNA gyrase comparable to that of ciprofloxacin. Molecular docking and density functional theory calculations were performed to explore the binding mode and study the reactivity of the promising compounds.\n                  <\/jats:p>","DOI":"10.1002\/ardp.202100266","type":"journal-article","created":{"date-parts":[[2021,11,8]],"date-time":"2021-11-08T07:23:05Z","timestamp":1636356185000},"update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":49,"title":["Design, synthesis, molecular modeling, and antimicrobial potential of novel 3\u2010[(1\n                    <i>H<\/i>\n                    \u2010pyrazol\u20103\u2010yl)imino]indolin\u20102\u2010one derivatives as DNA gyrase inhibitors"],"prefix":"10.1002","volume":"355","author":[{"ORCID":"https:\/\/orcid.org\/0000-0003-3195-8142","authenticated-orcid":false,"given":"Abdullah Y.","family":"Alzahrani","sequence":"first","affiliation":[{"name":"Department of Chemistry, Faculty of Science and Arts King Khalid University Mohail Assir Saudi Arabia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Yousry A.","family":"Ammar","sequence":"additional","affiliation":[{"name":"Department of Chemistry, Faculty of Science Al\u2010Azhar University Nasr City Cairo Egypt"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-4097-0899","authenticated-orcid":false,"given":"Mohamed A.","family":"Salem","sequence":"additional","affiliation":[{"name":"Department of Chemistry, Faculty of Science and Arts King Khalid University Mohail Assir Saudi Arabia"},{"name":"Department of Chemistry, Faculty of Science Al\u2010Azhar University Nasr City Cairo Egypt"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-9007-1029","authenticated-orcid":false,"given":"Mohammed","family":"Abu\u2010Elghait","sequence":"additional","affiliation":[{"name":"Department of Botany and Microbiology, Faculty of Science Al\u2010Azhar University Nasr City 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