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The design of these compounds was guided by the introduction of the isothiazoloquinolone motif. The three most active compounds in this series, <jats:bold>8\u201310<\/jats:bold>, demonstrated good antibacterial activity against methicillin\u2010sensitive <jats:italic>Staphylococcus aureus<\/jats:italic> and healthcare\u2010acquired methicillin\u2010resistant <jats:italic>Staphylococcus aureus<\/jats:italic> (MIC 0.62\u20136.3\u2009\u00b5g\/mL). Further, when these three active compounds were tested for their inhibitory effects on bacterial enzymes, compound <jats:bold>9<\/jats:bold> was the most effective agent exhibiting IC<jats:sub>50<\/jats:sub> values of 33.9 and 116.5\u2009\u03bcM in the <jats:italic>S. aureus<\/jats:italic> deoxyribonucleic acid (DNA) gyrase supercoiling and topoisomerase IV decatenation assays, respectively.<\/jats:p><\/jats:sec>","DOI":"10.1002\/ardp.201700029","type":"journal-article","created":{"date-parts":[[2017,4,21]],"date-time":"2017-04-21T08:38:59Z","timestamp":1492763939000},"source":"Crossref","is-referenced-by-count":15,"title":["Synthesis and Evaluation of Thiazolidine Amide and <i>N<\/i>\u2010Thiazolyl Amide Fluoroquinolone Derivatives"],"prefix":"10.1002","volume":"350","author":[{"given":"Isaac","family":"Garza","sequence":"first","affiliation":[{"name":"University of the Incarnate Word Feik School of Pharmacy San Antonio TX USA"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Miranda J.","family":"Wallace","sequence":"additional","affiliation":[{"name":"Department of Chemical Biology and Therapeutics St. Jude Children's Research Hospital Memphis TN USA"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Dinesh","family":"Fernando","sequence":"additional","affiliation":[{"name":"Department of Chemical Biology and Therapeutics St. Jude Children's Research Hospital Memphis TN USA"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Aman","family":"Singh","sequence":"additional","affiliation":[{"name":"Department of Chemical Biology and Therapeutics St. Jude Children's Research Hospital Memphis TN USA"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Richard E.","family":"Lee","sequence":"additional","affiliation":[{"name":"Department of Chemical Biology and Therapeutics St. Jude Children's Research Hospital Memphis TN USA"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Jason S.","family":"Gerding","sequence":"additional","affiliation":[{"name":"University of the Incarnate Word Feik School of Pharmacy San Antonio TX USA"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Cynthia","family":"Franklin","sequence":"additional","affiliation":[{"name":"University of the Incarnate Word Feik School of Pharmacy San Antonio TX USA"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-6491-7833","authenticated-orcid":false,"given":"Raghunandan","family":"Yendapally","sequence":"additional","affiliation":[{"name":"University of the Incarnate Word Feik School of Pharmacy San Antonio TX USA"}],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"311","published-online":{"date-parts":[[2017,4,21]]},"reference":[{"key":"e_1_2_7_2_1","doi-asserted-by":"publisher","DOI":"10.4065\/mcp.2010.0639"},{"key":"e_1_2_7_3_1","doi-asserted-by":"publisher","DOI":"10.1086\/319370"},{"key":"e_1_2_7_4_1","doi-asserted-by":"publisher","DOI":"10.1086\/321846"},{"key":"e_1_2_7_5_1","first-page":"379","volume":"14","author":"Chu D. 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