Tetrazole regioisomers in the development of nitro group-containing antitubercular agents

Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00216208%3A11160%2F15%3A10312842" target="_blank" >RIV/00216208:11160/15:10312842 - isvavai.cz</a>
Alternative codes found
RIV/60162694:G44__/15:43875343 RIV/00179906:_____/15:10312842
Result on the web
<a href="http://pubs.rsc.org/en/content/articlehtml/2015/md/c4md00301b" target="_blank" >http://pubs.rsc.org/en/content/articlehtml/2015/md/c4md00301b</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1039/c4md00301b" target="_blank" >10.1039/c4md00301b</a>

Result language
angličtina
Original language name
Tetrazole regioisomers in the development of nitro group-containing antitubercular agents
Original language description
Tetrazole derivatives containing nitro substituents have been identified as promising antitubercular agents. In this study, the antitubercular potency, selectivity and toxicity of tetrazole 1,5- and 2,5-regioisomers were examined. We prepared a series of1-and 2-alkyl-5-benzylsulfanyl-2H-tetrazoles and their selenium analogs with various nitro group substitutions. These 1,5-and 2,5-regioisomers were isolated and unambiguously identified using H-1 and/or C-13 NMR. Among the prepared compounds, 1-and 2-alkyl-5-[(3,5-dinitrobenzyl) sulfanyl]-2H-tetrazole derivatives and their selenium bioisosteres showed the highest antimycobacterial activity, with minimal inhibitory concentration (MIC) values of approximately 1 mu M (0.37-0.46 mu g mL(-1)) against Mycobacterium tuberculosis CNCTC My 331/88. The 2-alkyl regioisomers exhibited consistently higher antimycobacterial activity and lower in vitro toxicity against a mammalian cell line compared to the 1-alkyl isomers. The antimycobacterial activ
Czech name
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Czech description
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Type
J<sub>x</sub> - Unclassified - Peer-reviewed scientific article (Jimp, Jsc and Jost)
CEP classification
FR - Pharmacology and apothecary chemistry
OECD FORD branch
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Project
<a href="/en/project/GA14-08423S" target="_blank" >GA14-08423S: Structure-activity-toxicity relationships studies in the group of small-molecule compounds with antimycobacterial activity</a><br>
Continuities
S - Specificky vyzkum na vysokych skolach<br>I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Publication year
2015
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

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