{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,4,6]],"date-time":"2026-04-06T14:47:03Z","timestamp":1775486823451,"version":"3.50.1"},"reference-count":72,"publisher":"Wiley","issue":"10","license":[{"start":{"date-parts":[[2018,4,16]],"date-time":"2018-04-16T00:00:00Z","timestamp":1523836800000},"content-version":"vor","delay-in-days":0,"URL":"http:\/\/onlinelibrary.wiley.com\/termsAndConditions#vor"}],"funder":[{"DOI":"10.13039\/501100001809","name":"National Natural Science Foundation of China","doi-asserted-by":"publisher","award":["21672173"],"award-info":[{"award-number":["21672173"]}],"id":[{"id":"10.13039\/501100001809","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/501100001809","name":"National Natural Science Foundation of China","doi-asserted-by":"publisher","award":["21372186"],"award-info":[{"award-number":["21372186"]}],"id":[{"id":"10.13039\/501100001809","id-type":"DOI","asserted-by":"publisher"}]}],"content-domain":{"domain":["chemistry-europe.onlinelibrary.wiley.com"],"crossmark-restriction":true},"short-container-title":["ChemMedChem"],"published-print":{"date-parts":[[2018,5,23]]},"abstract":"<jats:title>Abstract<\/jats:title><jats:p>A series of benzimidazole\u2013quinolone hybrids as new potential antimicrobial agents were designed and synthesized. Bioactive assays indicated that some of the prepared compounds exhibited potent antibacterial and antifungal activities. Notably, 2\u2010fluorobenzyl derivative <jats:bold>5\u2009b<\/jats:bold> (ethyl 7\u2010chloro\u20106\u2010fluoro\u20101\u2010[[1\u2010[(2\u2010fluorophenyl)methyl]benzimidazol\u20102\u2010yl]methyl]\u20104\u2010oxo\u2010quinoline\u20103\u2010carboxylate) showed remarkable antimicrobial activity against resistant <jats:italic>Pseudomonas aeruginosa<\/jats:italic> and <jats:italic>Candida tropicalis<\/jats:italic> isolated from infected patients. Active molecule <jats:bold>5\u2009b<\/jats:bold> could not only rapidly kill the tested strains, but also exhibit low toxicity toward Hep\u20102 cells. It was more difficult to trigger the development of bacterial resistance of <jats:italic>P.\u2005aeruginosa<\/jats:italic> against <jats:bold>5\u2009b<\/jats:bold> than that against norfloxacin. Molecular docking demonstrated that <jats:bold>5\u2009b<\/jats:bold> could effectively bind with topoisomerase\u2005IV\u2013DNA complexes, and quantum chemical studies theoretically elucidated the good antimicrobial activity of compound <jats:bold>5\u2009b<\/jats:bold>. Preliminary experimental reaction mechanism exploration suggested that derivative <jats:bold>5\u2009b<\/jats:bold> could not intercalate into DNA isolated from drug\u2010resistant <jats:italic>P.\u2005aeruginosa<\/jats:italic>, but was able to cleave DNA effectively, which might further block DNA replication to exert powerful bioactivities. In addition, compound <jats:bold>5\u2009b<\/jats:bold> is a promising antibacterial agent with membrane disruption abilities.<\/jats:p>","DOI":"10.1002\/cmdc.201700739","type":"journal-article","created":{"date-parts":[[2018,3,7]],"date-time":"2018-03-07T06:16:41Z","timestamp":1520403401000},"page":"1004-1017","update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":59,"title":["Discovery of Benzimidazole\u2013Quinolone Hybrids as New Cleaving Agents toward Drug\u2010Resistant <i>Pseudomonas aeruginosa<\/i> DNA"],"prefix":"10.1002","volume":"13","author":[{"given":"Ya\u2010Nan","family":"Wang","sequence":"first","affiliation":[{"name":"Institute of Bioorganic &amp; Medicinal Chemistry, Key Laboratory of Applied Chemistry of Chongqing Municipality, School of Chemistry and Chemical Engineering Southwest University  Chongqing 400715 P.R. China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Rammohan R. Yadav","family":"Bheemanaboina","sequence":"additional","affiliation":[{"name":"Institute of Bioorganic &amp; Medicinal Chemistry, Key Laboratory of Applied Chemistry of Chongqing Municipality, School of Chemistry and Chemical Engineering Southwest University  Chongqing 400715 P.R. China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Wei\u2010Wei","family":"Gao","sequence":"additional","affiliation":[{"name":"Institute of Bioorganic &amp; Medicinal Chemistry, Key Laboratory of Applied Chemistry of Chongqing Municipality, School of Chemistry and Chemical Engineering Southwest University  Chongqing 400715 P.R. China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Jie","family":"Kang","sequence":"additional","affiliation":[{"name":"Institute of Bioorganic &amp; Medicinal Chemistry, Key Laboratory of Applied Chemistry of Chongqing Municipality, School of Chemistry and Chemical Engineering Southwest University  Chongqing 400715 P.R. China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Gui\u2010Xin","family":"Cai","sequence":"additional","affiliation":[{"name":"Institute of Bioorganic &amp; Medicinal Chemistry, Key Laboratory of Applied Chemistry of Chongqing Municipality, School of Chemistry and Chemical Engineering Southwest University  Chongqing 400715 P.R. China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-3233-5465","authenticated-orcid":false,"given":"Cheng\u2010He","family":"Zhou","sequence":"additional","affiliation":[{"name":"Institute of Bioorganic &amp; Medicinal Chemistry, Key Laboratory of Applied Chemistry of Chongqing Municipality, School of Chemistry and Chemical Engineering Southwest University  Chongqing 400715 P.R. 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