New 1,2,4-Triazole Potential Inhibitors of Mycobacterial Imidazoleglycerol-Phosphate Dehydratase (IGPD)
A number of new 5-aminomethyl-1,2,4-triazole-3-carboxamides, demonstrating high model affinity to the IGPD catalytic site comparable with that of the native substrate, were synthesized. The derivatives obtained were tested for antimicrobial potential against <i>M. smegmatis</i>, a specie...
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| Main Authors: | , , , , |
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| Format: | Article |
| Language: | English |
| Published: |
MDPI AG
2024-11-01
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| Series: | Chemistry Proceedings |
| Subjects: | |
| Online Access: | https://www.mdpi.com/2673-4583/16/1/67 |
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| Summary: | A number of new 5-aminomethyl-1,2,4-triazole-3-carboxamides, demonstrating high model affinity to the IGPD catalytic site comparable with that of the native substrate, were synthesized. The derivatives obtained were tested for antimicrobial potential against <i>M. smegmatis</i>, a species related to <i>M. tuberculosis</i>. During the initial antimicrobial activity evaluation in vitro, some compounds investigated inhibited microbial growth. Moreover, high binding energy values calculated for compounds/enzyme’s catalytic site complexes correlated with the compounds’ antimicrobial efficacy. This suggests that the probable biological action mechanism of new 5-aminomethyl-1,2,4-triazole-3-carboxamides may be based on their binding to the catalytic site of IGPD, which provides prerequisites for further study of this class of compounds as potential IGPD inhibitors. |
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| ISSN: | 2673-4583 |