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 against M. tuberculosis H37Rv.
RESULTS: Compound 8j was identified as antitubercular lead with MIC of 0.6 μg/ml against M. tuberculosis H37Rv. This compound was nontoxic to CHO-K1 cells and showed selectivity index of 39. Of note, 8j showed antitubercular activity against pre-extensively drug-resistant clinical isolate of Mycobacterium with MIC of 2 μg/ml.
CONCLUSION: This study provides potent antitubercular agent which can be further optimized to discover novel antibiotics.
| 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 vom: 31. März, Seite 499-510 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Makane, Vitthal B [VerfasserIn] |
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| Links: |
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| Themen: |
1,3,4-oxadiazole |
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| Anmerkungen: |
Date Completed 04.02.2020 Date Revised 04.02.2020 published: Print-Electronic Citation Status MEDLINE |
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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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| PPN (Katalog-ID): |
NLM295157062 |
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| 100 | 1 | |a Makane, Vitthal B |e verfasserin |4 aut | |
| 245 | 1 | 0 | |a Novel 1,3,4-oxadiazoles as antitubercular agents with limited activity against drug-resistant tuberculosis |
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| 500 | |a Date Completed 04.02.2020 | ||
| 500 | |a Date Revised 04.02.2020 | ||
| 500 | |a published: Print-Electronic | ||
| 500 | |a Citation Status MEDLINE | ||
| 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 | ||
| 520 | |a METHODOLOGY: A small library of 2-mercapto-1,3,4-oxadiazoles was synthesized using various acids. The compounds were evaluated for antituberculosis activity against M. tuberculosis H37Rv | ||
| 520 | |a RESULTS: Compound 8j was identified as antitubercular lead with MIC of 0.6 μg/ml against M. tuberculosis H37Rv. This compound was nontoxic to CHO-K1 cells and showed selectivity index of 39. Of note, 8j showed antitubercular activity against pre-extensively drug-resistant clinical isolate of Mycobacterium with MIC of 2 μg/ml | ||
| 520 | |a CONCLUSION: This study provides potent antitubercular agent which can be further optimized to discover novel antibiotics | ||
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a Research Support, Non-U.S. Gov't | |
| 650 | 4 | |a H37Rv | |
| 650 | 4 | |a 1,3,4-oxadiazoles | |
| 650 | 4 | |a antitubercular compounds | |
| 650 | 4 | |a drug-resistant tuberculosis | |
| 650 | 7 | |a Antitubercular Agents |2 NLM | |
| 650 | 7 | |a Oxadiazoles |2 NLM | |
| 650 | 7 | |a 1,3,4-oxadiazole |2 NLM | |
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| 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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