Design and synthesis of eugenol/isoeugenol glycoconjugates and other analogues as antifungal agents against Aspergillus fumigatus

RSC Medicinal Chemistry
2022.0

Abstract

Glycoconjugates are biologically significant molecules as they tend to serve a wide range of intra- and extra-cellular processes depending on their size and complexity. The secondary metabolites of the plant <i>Myristica fragrans</i>, eugenol and isoeugenol, have shown antifungal activities (IC<sub>50</sub> 1900 μM). Therefore, we envisioned that glycoconjugates based on these two scaffolds could prove to be potent antifungal agents. Triazole-containing compounds have shown prominent activities as antifungal agents. Based on this, we opined that a Cu(i) catalyzed click reaction could serve as the bridging tool between a eugenol/isoeugenol moiety and sugars to synthesize eugenol/isoeugenol based glycoconjugates. In our present work, we have coupled propargylated eugenol/isoeugenol and azido sugar to furnish eugenol/isoeugenol based glycoconjugates. In another approach, we have carried out hydroxylation of the double bond of eugenol and subsequent azidation of a primary alcohol followed by intramolecular coupling reactions leading to various other analogues. All the synthesized compounds were assayed against an opportunistic pathogenic fungus, <i>Aspergillus fumigatus</i>. Among the synthesized compounds, two analogues have exhibited significant antifungal activities with IC<sub>50</sub> values of 5.42 and 9.39 μM, respectively. The study suggested that these two analogues inhibit cell wall-associated melanin hydrophobicity along with the number of conidia. The synthesized compounds were found to be non-cytotoxic to an untransformed cell line.

Knowledge Graph

Similar Paper

Design and synthesis of eugenol/isoeugenol glycoconjugates and other analogues as antifungal agents against Aspergillus fumigatus
RSC Medicinal Chemistry 2022.0
Synthesis of sugars embodying conjugated carbonyl systems and related triazole derivatives from carboxymethyl glycoside lactones. Evaluation of their antimicrobial activity and toxicity
Bioorganic &amp; Medicinal Chemistry 2011.0
Efficient click chemistry towards novel 1H-1,2,3-triazole-tethered 4H-chromene−d-glucose conjugates: Design, synthesis and evaluation of in vitro antibacterial, MRSA and antifungal activities
European Journal of Medicinal Chemistry 2019.0
Synthesis and antifungal activity of the novel triazole compounds
MedChemComm 2013.0
New triazole derivatives as antifungal agents: Synthesis via click reaction, in vitro evaluation and molecular docking studies
Bioorganic &amp; Medicinal Chemistry Letters 2012.0
Azide-enolate 1,3-dipolar cycloaddition in the synthesis of novel triazole-based miconazole analogues as promising antifungal agents
European Journal of Medicinal Chemistry 2016.0
Design, synthesis and evaluation of aromatic heterocyclic derivatives as potent antifungal agents
European Journal of Medicinal Chemistry 2017.0
Synthesis of 2,3,6-trideoxy sugar triazole hybrids as potential new broad spectrum antimicrobial agents
European Journal of Medicinal Chemistry 2014.0
Synthesis of some diguanidino 1-methyl-2,5-diaryl-1H-pyrroles as antifungal agents
Bioorganic &amp; Medicinal Chemistry Letters 2005.0
A facile synthesis of novel miconazole analogues and the evaluation of their antifungal activity
European Journal of Medicinal Chemistry 2015.0