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Herein, an exploratory series of new 1,2,4\u2010triazole derivatives designed by amalgamation of arylpyrrole and 1,2,4\u2010triazole structural units via a hydrazone linkage is reported. The synthesised compounds were tested <jats:italic>in\u2005vitro<\/jats:italic> for their potential activity against <jats:italic>Mycobacterium tuberculosis<\/jats:italic> (MTB) H<jats:sub>37<\/jats:sub>Rv strain. The most promising compound 13 \u2013 the derivative without the benzene ring appended to the pyrrole unit displayed acceptable activity (MIC<jats:sub>90<\/jats:sub>=3.99\u2005\u03bcM) against MTB H<jats:sub>37<\/jats:sub>Rv, while other compounds from the series exhibited modest to weak antimycobacterial activity with MIC<jats:sub>90<\/jats:sub> values in the range between 7.0 and &gt;125\u2005\u03bcM. Furthermore, <jats:italic>in silico<\/jats:italic> results, predicated using the SwissADME web tool, show that the prepared compounds display desirable ADME profile with parameters within acceptable range.<\/jats:p>","DOI":"10.1002\/cmdc.202200572","type":"journal-article","created":{"date-parts":[[2023,1,8]],"date-time":"2023-01-08T22:13:50Z","timestamp":1673216030000},"update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":13,"title":["Hydrazone\u2010Tethered 5\u2010(Pyridin\u20104\u2010yl)\u20104<i>H<\/i>\u20101,2,4\u2010triazole\u20103\u2010thiol Hybrids: Synthesis, Characterisation, <i>in silico<\/i> ADME Studies, and <i>in\u2005vitro<\/i> Antimycobacterial Evaluation and Cytotoxicity"],"prefix":"10.1002","volume":"18","author":[{"ORCID":"https:\/\/orcid.org\/0000-0002-6180-5502","authenticated-orcid":false,"given":"Ogunyemi O.","family":"Oderinlo","sequence":"first","affiliation":[{"name":"Department of Chemistry Faculty of Science Rhodes University  Makhanda 6140 South Africa"},{"name":"Department of Chemistry Faculty of Science Federal University  Otuoke Bayelsa Nigeria"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Audrey","family":"Jordaan","sequence":"additional","affiliation":[{"name":"SAMRC\/NHLS\/UCT Molecular Mycobacteriology Research Unit Department of Pathology University of Cape Town  Cape Town, Observatory 7925 South Africa"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Ronnett","family":"Seldon","sequence":"additional","affiliation":[{"name":"SAMRC Drug Discovery and Development Unit University of Cape Town  Cape Town 7700 South Africa"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Michelle","family":"Isaacs","sequence":"additional","affiliation":[{"name":"Centre for Chemico- and Biomedicinal Research Rhodes University  Makhanda 6140 South Africa"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-4409-1955","authenticated-orcid":false,"given":"Heinrich C.","family":"Hoppe","sequence":"additional","affiliation":[{"name":"Centre for Chemico- and Biomedicinal Research Rhodes University  Makhanda 6140 South Africa"},{"name":"Department of Biochemistry and Microbiology Faculty of Science Rhodes University  Makhanda 6140 South Africa"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-4146-0930","authenticated-orcid":false,"given":"Digby F.","family":"Warner","sequence":"additional","affiliation":[{"name":"SAMRC\/NHLS\/UCT Molecular Mycobacteriology Research Unit Department of Pathology University of Cape Town  Cape Town, Observatory 7925 South Africa"},{"name":"Institute of Infectious Disease and Molecular Medicine University of Cape Town  Cape Town, Rondebosch 7701 South Africa"},{"name":"Wellcome Centre for Infectious Diseases Research in Africa (CIDRI-Africa) University of Cape Town  Cape Town, Rondebosch 7701 South Africa"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-1844-3614","authenticated-orcid":false,"given":"Matshawandile","family":"Tukulula","sequence":"additional","affiliation":[{"name":"School of Chemistry and Physics University of KwaZulu-NatalWestville Campus  Durban 4000 South Africa"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-0725-5738","authenticated-orcid":false,"given":"Setshaba D.","family":"Khanye","sequence":"additional","affiliation":[{"name":"Department of Chemistry Faculty of Science Rhodes University  Makhanda 6140 South Africa"},{"name":"Centre for Chemico- and Biomedicinal Research Rhodes University  Makhanda 6140 South Africa"},{"name":"Division of Pharmaceutical Chemistry Faculty of Pharmacy Rhodes University  Makhanda 6140 South Africa"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"311","published-online":{"date-parts":[[2023,1,30]]},"reference":[{"key":"e_1_2_8_1_1","unstructured":"CDC. 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