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- Title
4-Aminobenzoic Acid Derivatives: Converting Folate Precursor to Antimicrobial and Cytotoxic Agents.
- Authors
Krátký, Martin; KoneĈná, Klára; Janoušek, Jiří; Brablíková, Michaela; Jand'ourek, Ondřej; Trejtnar, František; Stolaříková, Jiřina; Vinšová, Jarmila
- Abstract
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.
- Subjects
ACID derivatives; AROMATIC aldehydes; ANTI-infective agents; SCHIFF bases; METHICILLIN-resistant staphylococcus aureus; FOLIC acid; ANTIBODY-dependent cell cytotoxicity; FORMYLATION
- Publication
Biomolecules (2218-273X), 2020, Vol 10, Issue 1, p1
- ISSN
2218-273X
- Publication type
Article
- DOI
10.3390/biom10010009