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3-Selenocyanate-indoles as new agents for the treatment of superficial and mucocutaneous infectionsElectronic supplementary information (ESI) available: Synthesis of 3-selenocyanate-indoles 4, tables of the mechanism of action, antibacterial susceptibility test, and HET-CAM assay. See DOI: 10.1039/c8nj04935a
The development of resistance to the current antifungal agents is an alarming problem. Therefore, the search for new molecules capable of combating fungi infections is imperative. This study presents the in vitro activities of a library of seven 3-selenocyanate-indoles against Candida spp. and derma...
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Main Authors: | , , , , , , , , , |
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Format: | Article |
Language: | English |
Online Access: | Get full text |
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Summary: | The development of resistance to the current antifungal agents is an alarming problem. Therefore, the search for new molecules capable of combating fungi infections is imperative. This study presents the
in vitro
activities of a library of seven 3-selenocyanate-indoles against
Candida
spp. and dermatophytes of the genera
Trichophyton
and
Microsporum
. The antifungal susceptibility of compounds
4a
and
4b
presented geometric mean values of 4.1 and 6.0 μg mL
−1
against
Candida
spp. and 1.2 and 2.2 μg mL
−1
against dermatophytes following the CLSI guidelines. The 3-selenocyanate-indole
4a
showed a fungicidal effect against the whole fungal panel. The toxicological results revealed that the selenocyanates
4a
and
4b
did not show mutagenicity or cause changes in the human leukocyte cells and were classified as non-irritant by the
ex vivo
HET-CAM test. The mechanism of action of the 3-selenocyanate-indoles has not been clearly elucidated. However, a genotoxic potential in higher concentrations, observed by the comet assay, leads us to believe that these molecules have their mechanism of action related to the nucleus of the fungal cells.
The development of resistance to the current antifungal agents is an alarming problem. |
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ISSN: | 1144-0546 1369-9261 |
DOI: | 10.1039/c8nj04935a |