{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,2,16]],"date-time":"2026-02-16T08:38:43Z","timestamp":1771231123702,"version":"3.50.1"},"reference-count":36,"publisher":"Wiley","issue":"10","license":[{"start":{"date-parts":[[2019,8,7]],"date-time":"2019-08-07T00:00:00Z","timestamp":1565136000000},"content-version":"vor","delay-in-days":0,"URL":"http:\/\/onlinelibrary.wiley.com\/termsAndConditions#vor"}],"content-domain":{"domain":["onlinelibrary.wiley.com"],"crossmark-restriction":true},"short-container-title":["Archiv der Pharmazie"],"published-print":{"date-parts":[[2019,10]]},"abstract":"<jats:title>Abstract<\/jats:title><jats:p>Antibiotic\u2010resistant bacteria continue to play an important role in human health and disease. Inventive strategies are necessary to develop new therapeutic leads to challenge drug\u2010resistance problems. From this perception, new quinoline hybrids bearing bioactive pharmacophores were synthesized. The newly synthesized compounds were evaluated for their in vitro antibacterial activity against nine bacterial pathogenic strains. The results revealed that most compounds exhibited good antibacterial activities. Seven compounds (<jats:bold>2b<\/jats:bold>, <jats:bold>3b<\/jats:bold>, <jats:bold>4<\/jats:bold>, <jats:bold>6<\/jats:bold>, <jats:bold>8b<\/jats:bold>, and <jats:bold>9c,d<\/jats:bold>) displayed enhanced activity against methicillin\u2010resistant <jats:italic>Staphylococcus aureus<\/jats:italic> compared to ampicillin. These compounds were subjected to an in vitro <jats:italic>S<\/jats:italic>. <jats:italic>aureus<\/jats:italic> DNA gyrase ATPase inhibition study, which revealed that compounds <jats:bold>8b<\/jats:bold>, <jats:bold>9c<\/jats:bold>, and <jats:bold>9d<\/jats:bold> showed the highest inhibitory activity with IC<jats:sub>50<\/jats:sub> values of 1.89, 2.73, and 2.14\u2009\u03bcM, respectively, comparable to novobiocin (IC<jats:sub>50<\/jats:sub>, 1.636\u2009\u03bcM). Compounds <jats:bold>2a\u2013c<\/jats:bold>, <jats:bold>3a<\/jats:bold>, <jats:bold>7c<\/jats:bold>, <jats:bold>9c,d<\/jats:bold>, and <jats:bold>10a,b<\/jats:bold> revealed half the potency of levofloxacin in inhibiting the growth of <jats:italic>Pseudomonas aeruginosa<\/jats:italic>. As an attempt to rationalize the observed antibacterial activity for the most active compounds <jats:bold>8b<\/jats:bold>, <jats:bold>9c<\/jats:bold>, and <jats:bold>9d<\/jats:bold>, molecular docking in the ATP binding site of <jats:italic>S<\/jats:italic>. <jats:italic>aureus<\/jats:italic> gyrase B was performed using Glide. Such compounds could be considered as promising scaffolds for the development of new potent antibacterial agents.<\/jats:p>","DOI":"10.1002\/ardp.201900086","type":"journal-article","created":{"date-parts":[[2019,8,7]],"date-time":"2019-08-07T10:24:12Z","timestamp":1565173452000},"update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":12,"title":["Synthesis, antibacterial evaluation, and DNA gyrase inhibition profile of some new quinoline hybrids"],"prefix":"10.1002","volume":"352","author":[{"ORCID":"https:\/\/orcid.org\/0000-0002-0278-0376","authenticated-orcid":false,"given":"Ola H.","family":"Rizk","sequence":"first","affiliation":[{"name":"Department of Pharmaceutical Chemistry Faculty of Pharmacy University of Alexandria Alexandria Egypt"},{"name":"Department of Pharmaceutical Chemistry, Faculty of Pharmacy &amp; Drug Manufacturing Pharos University in Alexandria Alexandria Egypt"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Mohamed G.","family":"Bekhit","sequence":"additional","affiliation":[{"name":"Department of Pharmaceutical Chemistry, Faculty of Pharmacy &amp; Drug Manufacturing Pharos University in Alexandria Alexandria Egypt"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Aly A. 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