4-Aminobenzoic Acid Derivatives: Converting Folate Precursor to Antimicrobial and Cytotoxic Agents
The result's identifiers
Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F71009396%3A_____%2F19%3AN0000029" target="_blank" >RIV/71009396:_____/19:N0000029 - isvavai.cz</a>
Alternative codes found
RIV/00216208:11160/20:10408638 RIV/71009396:_____/20:N0000010
Result on the web
<a href="https://www.mdpi.com/2218-273X/10/1/9/htm" target="_blank" >https://www.mdpi.com/2218-273X/10/1/9/htm</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.3390/biom10010009" target="_blank" >10.3390/biom10010009</a>
Alternative languages
Result language
angličtina
Original language name
4-Aminobenzoic Acid Derivatives: Converting Folate Precursor to Antimicrobial and Cytotoxic Agents
Original language description
4-aminobenzoic acid (PABA), an essential nutrient for many human pathogens, but dispensable for humans, and its derivatives have exhibited various biological activities. In this study, we combined two pharmacophores using a molecular hybridization approach: this vitamin-like molecule and various aromatic aldehydes, including salicylaldehydes and 5-nitrofurfural, via imine bond in one-step reaction. Resulting Schiff bases were screened as potential antimicrobial and cytotoxic agents. The simple chemical modification of non-toxic PABA resulted in constitution of antibacterial activity including inhibition of methicillin-resistant Staphylococcus aureus (minimum inhibitory concentrations, MIC, from 15.62 µM), moderate antimycobacterial activity (MIC ≥ 62.5 µM) and potent broad-spectrum antifungal properties (MIC of ≥ 7.81 µM). Some of the Schiff bases also exhibited notable cytotoxicity for cancer HepG2 cell line (IC50 ≥ 15.0 µM). Regarding aldehyde used for the derivatization of PABA, it is possible to tune up the particular activities and obtain derivatives with promising bioactivities.
Czech name
—
Czech description
—
Classification
Type
J<sub>imp</sub> - Article in a specialist periodical, which is included in the Web of Science database
CEP classification
—
OECD FORD branch
30107 - Medicinal chemistry
Result continuities
Project
Result was created during the realization of more than one project. More information in the Projects tab.
Continuities
V - Vyzkumna aktivita podporovana z jinych verejnych zdroju
Others
Publication year
2019
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů
Data specific for result type
Name of the periodical
BIOMOLECULES
ISSN
2218-273X
e-ISSN
—
Volume of the periodical
10
Issue of the periodical within the volume
9
Country of publishing house
CH - SWITZERLAND
Number of pages
20
Pages from-to
1-20
UT code for WoS article
000514863200070
EID of the result in the Scopus database
—