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Pharmaceuticals, volume 15, issue 5, pages 563

Antifungal Thiazolidines: Synthesis and Biological Evaluation of Mycosidine Congeners

Levshin Igor B 1
Simonov Alexander Y 1
Lavrenov Sergey N 1
Panov Alexey A 1
Grammatikova Natalia E 1
Ghazy Eslam S M O 2, 3, 4
Savin Nikita A 5
Erofeev Alexander S. 5
Publication typeJournal Article
Publication date2022-05-01
Journal: Pharmaceuticals
Quartile SCImago
Q1
Quartile WOS
Q2
Impact factor4.6
ISSN14248247
PubMed ID:  35631390
Drug Discovery
Pharmaceutical Science
Molecular Medicine
Abstract
Novel derivatives of Mycosidine (3,5-substituted thiazolidine-2,4-diones) are synthesized by Knoevenagel condensation and reactions of thiazolidines with chloroformates or halo-acetic acid esters. Furthermore, 5-Arylidene-2,4-thiazolidinediones and their 2-thioxo analogs containing halogen and hydroxy groups or di(benzyloxy) substituents in 5-benzylidene moiety are tested for antifungal activity in vitro. Some of the synthesized compounds exhibit high antifungal activity, both fungistatic and fungicidal, and lead to morphological changes in the Candida yeast cell wall. Based on the use of limited proteomic screening and toxicity analysis in mutants, we show that Mycosidine activity is associated with glucose transport. This suggests that this first-in-class antifungal drug has a novel mechanism of action that deserves further study.

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GOST |
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GOST Copy
Levshin I. B. et al. Antifungal Thiazolidines: Synthesis and Biological Evaluation of Mycosidine Congeners // Pharmaceuticals. 2022. Vol. 15. No. 5. p. 563.
GOST all authors (up to 50) Copy
Levshin I. B., Simonov A. Y., Lavrenov S. N., Panov A. A., Grammatikova N. E., Alexandrov A., Ghazy E. S. M. O., Savin N. A., Gorelkin P., Erofeev A. S., Polshakov V. I. Antifungal Thiazolidines: Synthesis and Biological Evaluation of Mycosidine Congeners // Pharmaceuticals. 2022. Vol. 15. No. 5. p. 563.
RIS |
Cite this
RIS Copy
TY - JOUR
DO - 10.3390/ph15050563
UR - https://doi.org/10.3390%2Fph15050563
TI - Antifungal Thiazolidines: Synthesis and Biological Evaluation of Mycosidine Congeners
T2 - Pharmaceuticals
AU - Levshin, Igor B
AU - Simonov, Alexander Y
AU - Panov, Alexey A
AU - Ghazy, Eslam S M O
AU - Savin, Nikita A
AU - Erofeev, Alexander S.
AU - Polshakov, Vladimir I
AU - Lavrenov, Sergey N
AU - Grammatikova, Natalia E
AU - Alexandrov, Alexander
AU - Gorelkin, Peter
PY - 2022
DA - 2022/05/01 00:00:00
PB - Multidisciplinary Digital Publishing Institute (MDPI)
SP - 563
IS - 5
VL - 15
PMID - 35631390
SN - 1424-8247
ER -
BibTex |
Cite this
BibTex Copy
@article{2022_Levshin,
author = {Igor B Levshin and Alexander Y Simonov and Alexey A Panov and Eslam S M O Ghazy and Nikita A Savin and Alexander S. Erofeev and Vladimir I Polshakov and Sergey N Lavrenov and Natalia E Grammatikova and Alexander Alexandrov and Peter Gorelkin},
title = {Antifungal Thiazolidines: Synthesis and Biological Evaluation of Mycosidine Congeners},
journal = {Pharmaceuticals},
year = {2022},
volume = {15},
publisher = {Multidisciplinary Digital Publishing Institute (MDPI)},
month = {may},
url = {https://doi.org/10.3390%2Fph15050563},
number = {5},
pages = {563},
doi = {10.3390/ph15050563}
}
MLA
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MLA Copy
Levshin, Igor B., et al. “Antifungal Thiazolidines: Synthesis and Biological Evaluation of Mycosidine Congeners.” Pharmaceuticals, vol. 15, no. 5, May. 2022, p. 563. https://doi.org/10.3390%2Fph15050563.
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