Enhancing the antimycobacterial efficacy of pyridine-4-carbohydrazide: linkage to additional antimicrobial agents via oxocarboxylic acids

Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F71009396%3A_____%2F25%3AN0000009" target="_blank" >RIV/71009396:_____/25:N0000009 - isvavai.cz</a>
Alternative codes found
RIV/00216208:11160/25:10486241
Result on the web
<a href="https://pubs.rsc.org/en/content/articlelanding/2025/md/d4md00663a" target="_blank" >https://pubs.rsc.org/en/content/articlelanding/2025/md/d4md00663a</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1039/d4md00663a" target="_blank" >10.1039/d4md00663a</a>

Result language
angličtina
Original language name
Enhancing the antimycobacterial efficacy of pyridine-4-carbohydrazide: linkage to additional antimicrobial agents via oxocarboxylic acids
Original language description
This study evaluates the antimycobacterial potential of novel "mutual" bioactive amides, combining pyridine-4-carbohydrazide (isoniazid, INH) with various antimicrobial agents (sulphonamides, 4-aminosalicylic acid, thiosemicarbazide, diphenyl (thio)ethers) via oxocarboxylic acids. The aim was to enhance activity against both drug-susceptible and multidrug-resistant (MDR) Mycobacterium tuberculosis and non-tuberculous strains, while overcoming drug resistance through dual-action mechanisms. Many derivatives exhibited potent antimycobacterial activity, with minimum inhibitory concentrations (MICs) as low as <= 0.25 mu M, outperforming INH, especially diphenyl (thio)ethers and biphenyl analogues. Additionally, the compounds were effective against M. kansasii (MICs <= 1 mu M) and inhibited MDR strains at higher concentrations (>= 8 mu M). The cytotoxicity assay indicated a favourable safety profile, with no significant haemolysis at 125 mu M, and some compounds were even protective. Selectivity for mycobacteria was confirmed by low inhibition of Gram-positive bacteria and inactivity against Gram-negative bacteria or fungi, highlighting the potential for further development as antimycobacterial agents.
Czech name
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Czech description
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Type
J<sub>imp</sub> - Article in a specialist periodical, which is included in the Web of Science database
CEP classification
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OECD FORD branch
10608 - Biochemistry and molecular biology

Project
Result was created during the realization of more than one project. More information in the Projects tab.
Continuities
P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)

Publication year
2025
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

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