Antifungal Activity of an Original Amino-Isocyanonaphthalene (ICAN) Compound Family: Promising Broad Spectrum Antifungals

Overview

Journal Molecules

Publisher MDPI

Specialty Biology

Date 2020 Feb 23

PMID 32085460

Citations 7

Authors

Miklos Nagy

Gabor Szeman-Nagy

Alexandra Kiss

Zsolt Laszlo Nagy

Laszlo Talas

David Racz

Laszlo Majoros

Zoltan Toth

Zsuzsa Mathene Szigeti

Istvan Pocsi

Sandor Keki

Affiliations

Soon will be listed here.

Abstract

Multiple drug resistant fungi pose a serious threat to human health, therefore the development of completely new antimycotics is of paramount importance. The in vitro antifungal activity of the original, 1-amino-5-isocyanonaphthalenes (ICANs) was evaluated against reference strains of clinically important species. Structure-activity studies revealed that the naphthalene core and the isocyano- together with the amino moieties are all necessary to exert antifungal activity. 1,1--dimethylamino-5-isocyanonaphthalene (DIMICAN), the most promising candidate, was tested further in vitro against clinical isolates of species, yielding a minimum inhibitory concentration (MIC) of 0.04-1.25 µg/mL. DIMICAN was found to be effective against intrinsically fluconazole resistant isolates, too. In vivo experiments were performed in a severly neutropenic murine model inoculated with a clinical strain of . Daily administration of 5 mg/kg DIMICAN intraperitoneally resulted in 80% survival even at day 13, whereas 100% of the control group died within six days. Based on these results, ICANs may become an effective clinical lead compound family against fungal pathogens.

Citing Articles

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