Design, Synthesis, and Biological Evaluation of Isothiosemicarbazones with Antimycobacterial Activity
The result's identifiers
Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61388963%3A_____%2F17%3A00478148" target="_blank" >RIV/61388963:_____/17:00478148 - isvavai.cz</a>
Alternative codes found
RIV/00216208:11160/17:10365149 RIV/00179906:_____/17:10365149 RIV/71009396:_____/17:N0000010
Result on the web
<a href="http://dx.doi.org/10.1002/ardp.201700020" target="_blank" >http://dx.doi.org/10.1002/ardp.201700020</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1002/ardp.201700020" target="_blank" >10.1002/ardp.201700020</a>
Alternative languages
Result language
angličtina
Original language name
Design, Synthesis, and Biological Evaluation of Isothiosemicarbazones with Antimycobacterial Activity
Original language description
A series of benzaldehyde and salicylaldehyde-S-benzylisothiosemicarbazones was synthesized and tested against 12 different strains of mycobacteria, Gram-positive and Gram-negative bacteria, and the significant selectivity toward mycobacteria was proved. Twenty-eight derivatives were evaluated for the inhibition of isocitrate lyase, which is a key enzyme of the glyoxylate cycle necessary for latent tuberculosis infection, and their iron-chelating properties were investigated. Two derivatives, 5-bromosalicylaldehyde-S-(4-fluorobenzyl)-isothiosemicarbazone and salicylaldehyde-S-(4-bromobenzyl)-isothiosemicarbazone, influenced the isocitrate lyase activity and caused a better inhibition at 10 mu mol/L than 3-nitropropionic acid, a standard inhibitor. The compounds were also found to act as exogenous chelators of iron, which is an obligate cofactor for many mycobacterial enzymes. Due to their low cytotoxicity, together with the activity against isocitrate lyase and the ability to sequester iron ions, the compounds belong to potential antibiotics with the main effect on mycobacteria.
Czech name
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Czech description
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Classification
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
10606 - Microbiology
Result continuities
Project
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Continuities
I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace
Others
Publication year
2017
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů
Data specific for result type
Name of the periodical
Archiv der Pharmazie
ISSN
0365-6233
e-ISSN
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Volume of the periodical
350
Issue of the periodical within the volume
8
Country of publishing house
DE - GERMANY
Number of pages
12
Pages from-to
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UT code for WoS article
000406714000003
EID of the result in the Scopus database
2-s2.0-85021182451