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- Title
A Novel Series of Acylhydrazones as Potential Anti-Candida Agents: Design, Synthesis, Biological Evaluation and In Silico Studies.
- Authors
Borcea, Anca-Maria; Marc, Gabriel; Ionuț, Ioana; Vodnar, Dan C.; Vlase, Laurian; Gligor, Felicia; Pricopie, Andreea; Pîrnău, Adrian; Tiperciuc, Brîndușa; Oniga, Ovidiu
- Abstract
In the context of an increased incidence of invasive fungal diseases, there is an imperative need of new antifungal drugs with improved activity and safety profiles. A novel series of acylhydrazones bearing a 1,4-phenylene-bisthiazole scaffold was designed based on an analysis of structures known to possess anti-Candida activity obtained from a literature review. Nine final compounds were synthesized and evaluated in vitro for their inhibitory activity against various strains of Candida spp. The anti-Candida activity assay revealed that some of the new compounds are as active as fluconazole against most of the tested strains. A molecular docking study was conducted in order to evaluate the binding poses towards lanosterol 14α-demethylase. An in silico ADMET analysis showed that the compounds possess drug-like properties and represent a biologically active framework that should be further optimized as potential hits.
- Subjects
MYCOSES; ANTIFUNGAL agents; CANDIDA; FLUCONAZOLE; MOLECULAR docking
- Publication
Molecules, 2019, Vol 24, Issue 1, p184
- ISSN
1420-3049
- Publication type
Article
- DOI
10.3390/molecules24010184