Novel 1,3,4-oxadiazoles as antitubercular agents with limited activity against drug-resistant tuberculosis
Aim:In recent times, heterocyclic chemotypes are being explored for the development of new antimycobacterials that target the drug-resistant tuberculosis. Here, we are disclosing the 5-substitued 2-mercapto-1,3,4-oxadiazoles as potent antitubercular agents.Methodology:A small library of 2-mercapto-1,3,4-oxadiazoles was synthesized using various acids. The compounds were evaluated for antituberculosis activity againstM. tuberculosisH37Rv.Results:Compound8jwas identified as antitubercular lead with MIC of 0.6g/ml againstM. tuberculosisH37Rv. This compound was nontoxic to CHO-K1 cells and showed selectivity index of 39. Of note,8jshowed antitubercular activity against pre-extensively drug-resistant clinical isolate ofMycobacteriumwith MIC of 2g/ml.Conclusion:This study provides potent antitubercular agent which can be further optimized to discover novel antibiotics. Aim: Methodology: M. tuberculosis Results: 8j M. tuberculosis 8j Mycobacterium Conclusion: Graphical abstract.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2019 |
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| Erschienen: |
2019 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:11 |
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| Enthalten in: |
Future medicinal chemistry - 11(2019), 6, Seite 499- |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Makane, Vitthal B [VerfasserIn] |
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| Links: |
FID Access [lizenzpflichtig] |
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| Umfang: |
1 Online-Ressource (12 p) |
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| doi: |
10.4155/fmc-2018-0378 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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KFL001069292 |
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| 520 | |a Aim:In recent times, heterocyclic chemotypes are being explored for the development of new antimycobacterials that target the drug-resistant tuberculosis. Here, we are disclosing the 5-substitued 2-mercapto-1,3,4-oxadiazoles as potent antitubercular agents.Methodology:A small library of 2-mercapto-1,3,4-oxadiazoles was synthesized using various acids. The compounds were evaluated for antituberculosis activity againstM. tuberculosisH37Rv.Results:Compound8jwas identified as antitubercular lead with MIC of 0.6g/ml againstM. tuberculosisH37Rv. This compound was nontoxic to CHO-K1 cells and showed selectivity index of 39. Of note,8jshowed antitubercular activity against pre-extensively drug-resistant clinical isolate ofMycobacteriumwith MIC of 2g/ml.Conclusion:This study provides potent antitubercular agent which can be further optimized to discover novel antibiotics. Aim: Methodology: M. tuberculosis Results: 8j M. tuberculosis 8j Mycobacterium Conclusion: Graphical abstract | ||
| 700 | 1 | |a Krishna, Vagolu Siva |e verfasserin |4 aut | |
| 700 | 1 | |a Krishna, Eruva Vamshi |e verfasserin |4 aut | |
| 700 | 1 | |a Shukla, Manjulika |e verfasserin |4 aut | |
| 700 | 1 | |a Mahizhaveni, Balakrishnan |e verfasserin |4 aut | |
| 700 | 1 | |a Misra, Sunil |e verfasserin |4 aut | |
| 700 | 1 | |a Chopra, Sidharth |e verfasserin |4 aut | |
| 700 | 1 | |a Sriram, Dharmarajan |e verfasserin |4 aut | |
| 700 | 1 | |a Azger Dusthackeer, Vijayan N |e verfasserin |4 aut | |
| 700 | 1 | |a Rode, Haridas B |e verfasserin |4 aut | |
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