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Preliminary evaluation indicated selectivity towards Mtb H37Rv, with no inhibition of non\u2010tubercular mycobacterial (NTM) &amp; bacterial pathogen panel. Out of 36 synthesized compounds, majority exhibited substantial inhibition of Mtb H37Rv (MIC 0.5\u20138\u2005\u03bcg\/mL). Cell viability test against Vero cells revealed no significant cytotoxicity. Further, screening against drug resistant strains (DR\u2010Mtb) found hit compound displaying promising potency (MIC 1\u20134\u2005\u03bcg\/mL). Structure optimization of the hit led to the identification of lead compound demonstrating potent inhibition of both drug\u2010susceptible Mtb (MIC 0.12\u2005\u03bcg\/mL) and drug\u2010resistant Mtb (MIC 0.25\u20130.5\u2005\u03bcg\/mL) along with a high selectivity index (SI) &gt;80. Taken together, with appreciable selectivity and potent activity, these chemotypes show prospect to be turned into a potential anti\u2010TB candidate.<\/jats:p>","DOI":"10.1002\/cbdv.202200324","type":"journal-article","created":{"date-parts":[[2022,6,2]],"date-time":"2022-06-02T15:34:14Z","timestamp":1654184054000},"update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":13,"title":["Exploration of Isoxazole\u2010Carboxylic Acid Methyl Ester Based 2\u2010Substituted Quinoline Derivatives as Promising Antitubercular Agents"],"prefix":"10.1002","volume":"19","author":[{"ORCID":"https:\/\/orcid.org\/0000-0002-0940-4584","authenticated-orcid":false,"given":"Santosh","family":"Kumar Sahoo","sequence":"first","affiliation":[{"name":"Department of chemical sciences National Institute of Pharmaceutical Education and Research (NIPER), Balanagar  Hyderabad 500037 India"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Mohammad","family":"Naiyaz Ahmad","sequence":"additional","affiliation":[{"name":"Division of Molecular Microbiology and Immunology CSIR-Central Drug Research Institute, Sector 10, Janakipuram Extension  Sitapur Road Lucknow 226031, UP India"},{"name":"AcSIR: Academy of Scientific and Innovative Research (AcSIR)  Ghaziabad 201002 India"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Grace","family":"Kaul","sequence":"additional","affiliation":[{"name":"Division of Molecular Microbiology and Immunology CSIR-Central Drug Research Institute, Sector 10, Janakipuram Extension  Sitapur Road Lucknow 226031, UP India"},{"name":"AcSIR: Academy of Scientific and Innovative Research (AcSIR)  Ghaziabad 201002 India"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-6671-2022","authenticated-orcid":false,"given":"Srinivas","family":"Nanduri","sequence":"additional","affiliation":[{"name":"Department of chemical sciences National Institute of Pharmaceutical Education and Research (NIPER), Balanagar  Hyderabad 500037 India"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-9014-1904","authenticated-orcid":false,"given":"Arunava","family":"Dasgupta","sequence":"additional","affiliation":[{"name":"Division of Molecular Microbiology and Immunology CSIR-Central Drug Research Institute, Sector 10, Janakipuram Extension  Sitapur Road Lucknow 226031, UP India"},{"name":"AcSIR: Academy of Scientific and Innovative Research (AcSIR)  Ghaziabad 201002 India"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-8823-6074","authenticated-orcid":false,"given":"Sidharth","family":"Chopra","sequence":"additional","affiliation":[{"name":"Division of Molecular Microbiology and Immunology CSIR-Central Drug Research Institute, Sector 10, Janakipuram Extension  Sitapur Road Lucknow 226031, UP India"},{"name":"AcSIR: Academy of Scientific and Innovative Research (AcSIR)  Ghaziabad 201002 India"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-9813-8694","authenticated-orcid":false,"given":"Venkata","family":"Madhavi Yaddanapudi","sequence":"additional","affiliation":[{"name":"Department of chemical sciences National Institute of Pharmaceutical Education and Research (NIPER), Balanagar  Hyderabad 500037 India"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"311","published-online":{"date-parts":[[2022,6,23]]},"reference":[{"key":"e_1_2_8_1_1","unstructured":"Global tuberculosis report WHO Geneva 2021. https:\/\/www.who.int\/publications\/i\/item\/9789240037021"},{"key":"e_1_2_8_2_1","doi-asserted-by":"crossref","unstructured":"G.\u2005M. 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