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Herein, we report the synthesis and bioevaluation of 30 piperazinyl<jats:bold>\u2010<\/jats:bold>benzothiazinone\u2010based quinoline hybrids as prospective anti\u2010TB agents. Preliminary evaluation revealed 24\/30 compounds exhibiting substantial activity (minimum inhibitory concentration [MIC]\u2009=\u20090.06\u20131\u2009\u00b5g\/ml) against <jats:italic>Mycobacterium tuberculosis<\/jats:italic>\u00a0(Mtb) H37Rv. Cytotoxicity analysis against Vero cells found these to be devoid of any significant toxicity, with the majority displaying a selectivity index\u00a0of &gt;80. Furthermore, potent nontoxic compounds, when screened against clinical isolates of drug\u2010resistant\u00a0Mtb strains, demonstrated equipotent inhibition with MIC values of 0.03\u20130.25\u2009\u00b5g\/ml. A time\u2010kill study identified a lead compound exhibiting concentration\u2010dependent bactericidal activity, with 10\u00d7 MIC completely eliminating Mtb bacilli within 7 days. Along with acceptable aqueous solubility and microsomal stability, the optimum active compounds of the series manifested all desirable traits of a promising antimycobacterial candidate.<\/jats:p>","DOI":"10.1002\/ardp.202200168","type":"journal-article","created":{"date-parts":[[2022,7,25]],"date-time":"2022-07-25T11:49:42Z","timestamp":1658749782000},"update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":13,"title":["Bioevaluation of quinoline\u20104\u2010carbonyl derivatives of piperazinyl\u2010benzothiazinones as promising antimycobacterial agents"],"prefix":"10.1002","volume":"355","author":[{"ORCID":"https:\/\/orcid.org\/0000-0002-0940-4584","authenticated-orcid":false,"given":"Santosh K.","family":"Sahoo","sequence":"first","affiliation":[{"name":"Department of Chemical Sciences National Institute of Pharmaceutical Education and Research (NIPER)  Hyderabad Telangana India"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Siva N. 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