{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,10,8]],"date-time":"2026-10-08T04:57:25Z","timestamp":1791435445198,"version":"4.3.3"},"reference-count":87,"publisher":"Wiley","issue":"2","license":[{"start":{"date-parts":[[2022,10,28]],"date-time":"2022-10-28T00:00:00Z","timestamp":1666915200000},"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":["Chem Biol Drug Des"],"published-print":{"date-parts":[[2023,2]]},"abstract":"<jats:title>Abstract<\/jats:title><jats:p>This study aimed to synthesize new potent quinoline derivatives based on hydrazone moieties and evaluate their antimicrobial activity. The newly synthesized hydrazono\u2010quinoline derivatives <jats:bold>2<\/jats:bold>, <jats:bold>5a<\/jats:bold>, <jats:bold>9<\/jats:bold>, and <jats:bold>10b<\/jats:bold> showed the highest antimicrobial activity with MIC values \u22641.0\u2009\u03bcg\/ml against bacteria and \u22648.0\u2009\u03bcg\/ml against the fungi. Further, these derivatives exhibited bactericidal and fungicidal effects with MBC\/MIC and MFC\/MIC ratio \u22644. Surprisingly, the most active compounds displayed good inhibition to biofilm formation with MBEC values ranging between (40.0\u2009\u00b1\u200910.0 \u2013 230.0\u2009\u00b1\u200931.0) and (67.0\u2009\u00b1\u200924.0 \u2013 347.0\u2009\u00b1\u200915.0) \u03bcg\/ml against <jats:italic>Staphylococcus aureus<\/jats:italic> and <jats:italic>Pseudomonas aeruginosa<\/jats:italic>, respectively. The hemolytic assays confirmed that the hydrazono\u2010quinoline derivatives are non\u2010toxic with low % lysis values ranging from 4.62% to 14.4% at a 1.0\u2009mg\/ml concentration. Besides, compound <jats:bold>5a<\/jats:bold> exhibited the lowest hemolytic activity value of ~4.62%. Furthermore, the study suggests that the hydrazono\u2010quinoline analogs exert their antibacterial activity as dual inhibitors for DNA gyrase and DNA topoisomerase IV enzymes with IC<jats:sub>50<\/jats:sub> values ranging between (4.56\u2009\u00b1\u20090.3 \u2013 21.67\u2009\u00b1\u20090.45) and (6.77\u2009\u00b1\u20090.4 \u2013 20.41\u2009\u00b1\u20090.32) \u03bcM, respectively. Additionally, the recent work advocated that compound <jats:bold>5a<\/jats:bold> showed the reference SAL at the \u0263\u2010radiation dose of 10.0 kGy in the sterilization process without affecting its chemical structure. Finally, the <jats:italic>in silico<\/jats:italic> drug\u2010likeness, toxicity properties, and molecular docking simulation were performed. Besides, the result exhibited good oral\u2010bioavailability, lower toxicity prediction, and lower binding energy with good binding mode rather than the positive control.<\/jats:p>","DOI":"10.1111\/cbdd.14154","type":"journal-article","created":{"date-parts":[[2022,10,28]],"date-time":"2022-10-28T14:05:42Z","timestamp":1666965942000},"page":"245-270","update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":35,"title":["Development and radiosterilization of new hydrazono\u2010quinoline hybrids as <scp>DNA<\/scp> gyrase and topoisomerase <scp>IV<\/scp> inhibitors: Antimicrobial and hemolytic activities against uropathogenic isolates with molecular docking study"],"prefix":"10.1111","volume":"101","author":[{"ORCID":"https:\/\/orcid.org\/0000-0001-8989-4394","authenticated-orcid":false,"given":"Yousry A.","family":"Ammar","sequence":"first","affiliation":[{"name":"Department of Chemistry, Faculty of Science (Boys) Al\u2010Azhar University  Nasr City Cairo Egypt"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Jehan A.","family":"Micky","sequence":"additional","affiliation":[{"name":"Department of Chemistry, Faculty of Science (Girls) Al\u2010Azhar University  Nasr City, Cairo Egypt"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-1962-8629","authenticated-orcid":false,"given":"Dina S.","family":"Aboul\u2010Magd","sequence":"additional","affiliation":[{"name":"Drug Radiation Research Department, National Center for Radiation Research and Technology (NCRRT) Egyptian Atomic Energy Authority  Egypt"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Sondos M. A.","family":"Abd El\u2010Hafez","sequence":"additional","affiliation":[{"name":"Department of Chemistry, Faculty of Science (Girls) Al\u2010Azhar University  Nasr City, Cairo Egypt"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Sadia A.","family":"Hessein","sequence":"additional","affiliation":[{"name":"Department of Chemistry, Faculty of Science (Girls) Al\u2010Azhar University  Nasr City, Cairo Egypt"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Abeer M.","family":"Ali","sequence":"additional","affiliation":[{"name":"Department of Chemistry, Faculty of Science (Girls) Al\u2010Azhar University  Nasr City, Cairo Egypt"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-8542-7465","authenticated-orcid":false,"given":"Ahmed","family":"Ragab","sequence":"additional","affiliation":[{"name":"Department of Chemistry, Faculty of Science (Boys) Al\u2010Azhar University  Nasr City Cairo Egypt"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"311","published-online":{"date-parts":[[2022,10,28]]},"reference":[{"key":"e_1_2_7_2_1","doi-asserted-by":"publisher","DOI":"10.1155\/2014\/760434"},{"key":"e_1_2_7_3_1","doi-asserted-by":"publisher","DOI":"10.1080\/00397911.2017.1330961"},{"key":"e_1_2_7_4_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.ejmech.2017.07.004"},{"key":"e_1_2_7_5_1","doi-asserted-by":"publisher","DOI":"10.3390\/molecules25194565"},{"key":"e_1_2_7_6_1","doi-asserted-by":"publisher","DOI":"10.1021\/cb400592n"},{"key":"e_1_2_7_7_1","doi-asserted-by":"publisher","DOI":"10.1021\/acsomega.1c05801"},{"key":"e_1_2_7_8_1","doi-asserted-by":"publisher","DOI":"10.3390\/ph11010003"},{"key":"e_1_2_7_9_1","doi-asserted-by":"publisher","DOI":"10.3390\/molecules201119655"},{"key":"e_1_2_7_10_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.sjbs.2020.09.061"},{"key":"e_1_2_7_11_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.bioorg.2021.105571"},{"key":"e_1_2_7_12_1","doi-asserted-by":"publisher","DOI":"10.1002\/ardp.202100266"},{"key":"e_1_2_7_13_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.molstruc.2021.130748"},{"key":"e_1_2_7_14_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.bioorg.2020.103841"},{"key":"e_1_2_7_15_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.bioorg.2020.104164"},{"key":"e_1_2_7_16_1","doi-asserted-by":"publisher","DOI":"10.1038\/nrmicro2319"},{"key":"e_1_2_7_17_1","doi-asserted-by":"publisher","DOI":"10.1080\/00325481.2019.1680052"},{"key":"e_1_2_7_18_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.ebiom.2021.103652"},{"key":"e_1_2_7_19_1","doi-asserted-by":"crossref","first-page":"1518","DOI":"10.5380\/acd.v11i2.21366","article-title":"Tests in vitro and in vivo used in the toxicological screening of natural products","volume":"11","author":"Bednarczuk V. O.","year":"2010","journal-title":"Vis\u00e3o Acad\u00eamica"},{"key":"e_1_2_7_20_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.fct.2017.03.033"},{"key":"e_1_2_7_21_1","doi-asserted-by":"publisher","DOI":"10.1517\/14656566.2013.778827"},{"key":"e_1_2_7_22_1","doi-asserted-by":"publisher","DOI":"10.5772\/61052"},{"key":"e_1_2_7_23_1","doi-asserted-by":"publisher","DOI":"10.1007\/s00253\u2010011\u20103557\u2010z"},{"key":"e_1_2_7_24_1","doi-asserted-by":"publisher","DOI":"10.1371\/journal.pone.0105217"},{"key":"e_1_2_7_25_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.eimc.2016.11.005"},{"key":"e_1_2_7_26_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.ejmech.2004.06.007"},{"key":"e_1_2_7_27_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.ejmech.2020.112326"},{"key":"e_1_2_7_28_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.bioorg.2021.104803"},{"key":"e_1_2_7_29_1","doi-asserted-by":"publisher","DOI":"10.3390\/biomedicines10030722"},{"key":"e_1_2_7_30_1","doi-asserted-by":"publisher","DOI":"10.3390\/ph15030376"},{"key":"e_1_2_7_31_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.molstruc.2021.131314"},{"key":"e_1_2_7_32_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.bmcl.2009.12.045"},{"key":"e_1_2_7_33_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.molstruc.2021.132004"},{"key":"e_1_2_7_34_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.bioorg.2020.103951"},{"key":"e_1_2_7_35_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.molstruc.2021.130317"},{"key":"e_1_2_7_36_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.molstruc.2022.133028"},{"key":"e_1_2_7_37_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.bioorg.2021.105300"},{"key":"e_1_2_7_38_1","doi-asserted-by":"publisher","DOI":"10.1038\/nrmicro3432"},{"key":"e_1_2_7_39_1","doi-asserted-by":"publisher","DOI":"10.1038\/nrurol.2010.190"},{"key":"e_1_2_7_40_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.idc.2013.09.003"},{"key":"e_1_2_7_41_1","first-page":"126","article-title":"In vitro antibacterial activity of crinum Purpurascens herb leaf extract against the Salmonella species causing typhoid fever and its toxicological evaluation","volume":"34","author":"Gatsing D.","year":"2009","journal-title":"Iranian Journal of Medical Sciences"},{"key":"e_1_2_7_42_1","doi-asserted-by":"publisher","DOI":"10.1111\/nyas.13739"},{"key":"e_1_2_7_43_1","doi-asserted-by":"publisher","DOI":"10.1002\/jhet.3131"},{"key":"e_1_2_7_44_1","doi-asserted-by":"publisher","DOI":"10.3390\/ijms17091499"},{"key":"e_1_2_7_45_1","doi-asserted-by":"publisher","DOI":"10.1080\/17518253.2019.1710268"},{"key":"e_1_2_7_46_1","doi-asserted-by":"publisher","DOI":"10.3390\/molecules25112593"},{"key":"e_1_2_7_47_1","doi-asserted-by":"publisher","DOI":"10.1007\/s13738\u2010021\u201002319\u20104"},{"key":"e_1_2_7_48_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.bioorg.2021.105339"},{"key":"e_1_2_7_49_1","doi-asserted-by":"publisher","DOI":"10.1002\/aoc.6508"},{"key":"e_1_2_7_50_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.dyepig.2021.109504"},{"key":"e_1_2_7_51_1","doi-asserted-by":"publisher","DOI":"10.5772\/57353"},{"key":"e_1_2_7_52_1","doi-asserted-by":"publisher","DOI":"10.1002\/cmdc.200690024"},{"key":"e_1_2_7_53_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.tim.2020.03.016"},{"key":"e_1_2_7_54_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.arabjc.2021.103396"},{"key":"e_1_2_7_55_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.arabjc.2020.10.026"},{"key":"e_1_2_7_56_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.biopha.2014.10.007"},{"key":"e_1_2_7_57_1","doi-asserted-by":"publisher","DOI":"10.1080\/07391102.2021.1989036"},{"key":"e_1_2_7_58_1","doi-asserted-by":"publisher","DOI":"10.1016\/S1473\u20103099(20)30330\u20103"},{"key":"e_1_2_7_59_1","doi-asserted-by":"publisher","DOI":"10.1016\/S0167\u20104781(98)00126\u20102"},{"key":"e_1_2_7_60_1","doi-asserted-by":"publisher","DOI":"10.3390\/pathogens8010012"},{"key":"e_1_2_7_61_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.ejmech.2016.07.028"},{"key":"e_1_2_7_62_1","doi-asserted-by":"publisher","DOI":"10.1002\/ardp.202000103"},{"key":"e_1_2_7_63_1","doi-asserted-by":"publisher","DOI":"10.1038\/nrurol.2010.101"},{"key":"e_1_2_7_64_1","doi-asserted-by":"publisher","DOI":"10.1002\/jhet.3040"},{"key":"e_1_2_7_65_1","first-page":"e110","article-title":"Role of medicinal chemist in the modern drug discovery and development","volume":"2","author":"Patil S. A.","year":"2012","journal-title":"Org. Chem. Curr. Ress"},{"key":"e_1_2_7_66_1","doi-asserted-by":"publisher","DOI":"10.1039\/c9md00120d"},{"key":"e_1_2_7_67_1","doi-asserted-by":"publisher","DOI":"10.1002\/ddr.21960"},{"key":"e_1_2_7_68_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.compbiomed.2022.105473"},{"key":"e_1_2_7_69_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.arabjc.2021.103497"},{"key":"e_1_2_7_70_1","doi-asserted-by":"publisher","DOI":"10.3390\/antibiotics10020162"},{"key":"e_1_2_7_71_1","doi-asserted-by":"publisher","DOI":"10.1007\/s13738\u2010020\u201001944\u20109"},{"key":"e_1_2_7_72_1","doi-asserted-by":"publisher","DOI":"10.1080\/10406638.2021.2015402"},{"key":"e_1_2_7_73_1","doi-asserted-by":"publisher","DOI":"10.1007\/s13738\u2010022\u201002575\u2010y"},{"key":"e_1_2_7_74_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.ejmech.2019.111977"},{"key":"e_1_2_7_75_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.bioorg.2020.103619"},{"key":"e_1_2_7_76_1","doi-asserted-by":"publisher","DOI":"10.1021\/acsmedchemlett.5b00169"},{"key":"e_1_2_7_77_1","doi-asserted-by":"publisher","DOI":"10.1080\/17518253.2021.1893392"},{"key":"e_1_2_7_78_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.mtchem.2020.100349"},{"key":"e_1_2_7_79_1","doi-asserted-by":"publisher","DOI":"10.1038\/s41585\u2010018\u20100106\u2010x"},{"key":"e_1_2_7_80_1","doi-asserted-by":"publisher","DOI":"10.1016\/0165-6147(94)90033-7"},{"key":"e_1_2_7_81_1","doi-asserted-by":"publisher","DOI":"10.3389\/fchem.2022.911453"},{"key":"e_1_2_7_82_1","doi-asserted-by":"publisher","DOI":"10.1093\/jac\/dkn133"},{"key":"e_1_2_7_83_1","first-page":"863","volume-title":"Chapter 1211: Sterilization and Sterility Assurance of Compendial Articles","author":"USP 35","year":"2012"},{"key":"e_1_2_7_84_1","doi-asserted-by":"publisher","DOI":"10.1038\/nrm831"},{"key":"e_1_2_7_85_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.bioorg.2021.104794"},{"key":"e_1_2_7_86_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.molstruc.2020.128966"},{"key":"e_1_2_7_87_1","volume-title":"M100: Performance Standards for Antimicrobial Susceptibility Testing. CLSI Supplement","author":"Wayne P. A.","year":"2018"},{"key":"e_1_2_7_88_1","volume-title":"Methods for dilution antimicrobial susceptibility tests for bacteria that grow aerobically. CLSI supplement M07","author":"Wayne P. A.","year":"2018"}],"container-title":["Chemical Biology &amp; Drug Design"],"original-title":[],"language":"en","link":[{"URL":"https:\/\/onlinelibrary.wiley.com\/doi\/pdf\/10.1111\/cbdd.14154","content-type":"application\/pdf","content-version":"vor","intended-application":"text-mining"},{"URL":"https:\/\/onlinelibrary.wiley.com\/doi\/full-xml\/10.1111\/cbdd.14154","content-type":"application\/xml","content-version":"vor","intended-application":"text-mining"},{"URL":"https:\/\/onlinelibrary.wiley.com\/doi\/pdf\/10.1111\/cbdd.14154","content-type":"unspecified","content-version":"vor","intended-application":"similarity-checking"}],"deposited":{"date-parts":[[2023,8,20]],"date-time":"2023-08-20T01:12:02Z","timestamp":1692493922000},"score":1,"resource":{"primary":{"URL":"https:\/\/onlinelibrary.wiley.com\/doi\/10.1111\/cbdd.14154"}},"subtitle":[],"short-title":[],"issued":{"date-parts":[[2022,10,28]]},"references-count":87,"journal-issue":{"issue":"2","published-print":{"date-parts":[[2023,2]]}},"alternative-id":["10.1111\/cbdd.14154"],"URL":"https:\/\/doi.org\/10.1111\/cbdd.14154","archive":["Portico"],"relation":{},"ISSN":["1747-0277","1747-0285"],"issn-type":[{"value":"1747-0277","type":"print"},{"value":"1747-0285","type":"electronic"}],"subject":[],"published":{"date-parts":[[2022,10,28]]},"assertion":[{"value":"2022-04-02","order":0,"name":"received","label":"Received","group":{"name":"publication_history","label":"Publication History"}},{"value":"2022-10-09","order":1,"name":"accepted","label":"Accepted","group":{"name":"publication_history","label":"Publication History"}},{"value":"2022-10-28","order":2,"name":"published","label":"Published","group":{"name":"publication_history","label":"Publication History"}}]}}