{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,6,6]],"date-time":"2026-06-06T07:58:31Z","timestamp":1780732711861,"version":"3.54.1"},"reference-count":59,"publisher":"MDPI AG","issue":"12","license":[{"start":{"date-parts":[[2020,12,15]],"date-time":"2020-12-15T00:00:00Z","timestamp":1607990400000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"funder":[{"name":"The National Science Centre","award":["2014\/14\/E\/ST5\/00577"],"award-info":[{"award-number":["2014\/14\/E\/ST5\/00577"]}]},{"name":"Institute of Medical Biology Polish Academy of Sciences","award":["T-76"],"award-info":[{"award-number":["T-76"]}]}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Pharmaceuticals"],"abstract":"<jats:p>Tuberculosis (TB) is a severe infectious disease with high mortality and morbidity. The emergence of drug-resistant TB has increased the challenge to eliminate this disease. Isoniazid (INH) remains the key and effective component in the therapeutic regimen recommended by World Health Organization (WHO). A series of isoniazid-carborane derivatives containing 1,2-dicarba-closo-dodecaborane, 1,7-dicarba-closo-dodecaborane, 1,12-dicarba-closo-dodecaborane, or 7,8-dicarba-nido-undecaborate anion were synthesized for the first time. The compounds were tested in vitro against the Mycobacterium tuberculosis (Mtb) H37Rv strain and its mutant (\u0394katG) defective in the synthesis of catalase-peroxidase (KatG). N\u2032-((7,8-dicarba-nido-undecaboranyl)methylidene)isonicotinohydrazide (16) showed the highest activity against the wild-type Mtb strain. All hybrids could inhibit the growth of the \u0394katG mutant in lower concentrations than INH. N\u2032-([(1,12-dicarba-closo-dodecaboran-1yl)ethyl)isonicotinohydrazide (25) exhibited more than 60-fold increase in activity against Mtb \u0394katG as compared to INH. This compound was also found to be noncytotoxic up to a concentration four times higher than the minimum inhibitory concentration 99% (MIC99) value.<\/jats:p>","DOI":"10.3390\/ph13120465","type":"journal-article","created":{"date-parts":[[2020,12,15]],"date-time":"2020-12-15T09:12:57Z","timestamp":1608023577000},"page":"465","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":24,"title":["Novel Isoniazid-Carborane Hybrids Active In Vitro against Mycobacterium tuberculosis"],"prefix":"10.3390","volume":"13","author":[{"given":"Daria","family":"R\u00f3\u017cycka","sequence":"first","affiliation":[{"name":"Institute of Medical Biology, Polish Academy of Sciences, 106 Lodowa St., 93-232 Lodz, Poland"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Ma\u0142gorzata","family":"Korycka-Macha\u0142a","sequence":"additional","affiliation":[{"name":"Institute of Medical Biology, Polish Academy of Sciences, 106 Lodowa St., 93-232 Lodz, Poland"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-7443-9348","authenticated-orcid":false,"given":"Anna","family":"\u017baczek","sequence":"additional","affiliation":[{"name":"Institute of Medical Sciences, Medical College, University of Rzeszow, 2A Kopisto Avenue, 35-959 Rzeszow, Poland"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-1427-884X","authenticated-orcid":false,"given":"Jaros\u0142aw","family":"Dziadek","sequence":"additional","affiliation":[{"name":"Institute of Medical Biology, Polish Academy of Sciences, 106 Lodowa St., 93-232 Lodz, Poland"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Dorota","family":"Gurda","sequence":"additional","affiliation":[{"name":"Institute of Bioorganic Chemistry, Polish Academy of Sciences, 12\/14Z. Noskowskiego St., 61-704 Poznan, Poland"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Marta","family":"Orlicka-P\u0142ocka","sequence":"additional","affiliation":[{"name":"Institute of Bioorganic Chemistry, Polish Academy of Sciences, 12\/14Z. Noskowskiego St., 61-704 Poznan, Poland"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Eliza","family":"Wyszko","sequence":"additional","affiliation":[{"name":"Institute of Bioorganic Chemistry, Polish Academy of Sciences, 12\/14Z. Noskowskiego St., 61-704 Poznan, Poland"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Katarzyna","family":"Biniek-Antosiak","sequence":"additional","affiliation":[{"name":"Institute of Bioorganic Chemistry, Polish Academy of Sciences, 12\/14Z. 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Noskowskiego St., 61-704 Poznan, Poland"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-4628-9017","authenticated-orcid":false,"given":"Agnieszka B.","family":"Olejniczak","sequence":"additional","affiliation":[{"name":"Institute of Medical Biology, Polish Academy of Sciences, 106 Lodowa St., 93-232 Lodz, Poland"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"1968","published-online":{"date-parts":[[2020,12,15]]},"reference":[{"key":"ref_1","doi-asserted-by":"crossref","first-page":"2060","DOI":"10.1513\/AnnalsATS.201607-567CME","article-title":"Treatment of drug-susceptible tuberculosis","volume":"13","author":"Lyons","year":"2016","journal-title":"Ann. Am. Thorac. Soc."},{"key":"ref_2","doi-asserted-by":"crossref","unstructured":"Fernandes, G.F.d.S., Chin, C.M., and Dos Santos, J.L. (2017). Advances in drug discovery of new antitubercular multidrug-resistant compounds. 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