Open Access
A Novel Series of [1,2,4]Triazolo[4,3-a]Pyridine Sulfonamides as Potential Antimalarial Agents: In Silico Studies, Synthesis and In Vitro Evaluation
Тип публикации: Journal Article
Дата публикации: 2020-09-30
PubMed ID:
33007887
Organic Chemistry
Drug Discovery
Physical and Theoretical Chemistry
Pharmaceutical Science
Molecular Medicine
Analytical Chemistry
Chemistry (miscellaneous)
Краткое описание
For the development of new and potent antimalarial drugs, we designed the virtual library with three points of randomization of novel [1,2,4]triazolo[4,3-a]pyridines bearing a sulfonamide fragment. The library of 1561 compounds has been investigated by both virtual screening and molecular docking methods using falcipain-2 as a target enzyme. 25 chosen hits were synthesized and evaluated for their antimalarial activity in vitro against Plasmodium falciparum. 3-Ethyl-N-(3-fluorobenzyl)-N-(4-methoxyphenyl)-[1,2,4]triazolo[4,3-a]pyridine-6-sulfonamide and 2-(3-chlorobenzyl)-8-(piperidin-1-ylsulfonyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one showed in vitro good antimalarial activity with inhibitory concentration IC50 = 2.24 and 4.98 μM, respectively. This new series of compounds may serve as a starting point for future antimalarial drug discovery programs.
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19
Всего цитирований:
19
Цитирований c 2025:
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(36.84%)
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ГОСТ
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Karpina V. R. et al. A Novel Series of [1,2,4]Triazolo[4,3-a]Pyridine Sulfonamides as Potential Antimalarial Agents: In Silico Studies, Synthesis and In Vitro Evaluation // Molecules. 2020. Vol. 25. No. 19. p. 4485.
ГОСТ со всеми авторами (до 50)
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Karpina V. R., Kovalenko S. S., Kovalenko S. M., Drushlyak O. G., Bunyatyan N. D., Georgiyants V. A., Ivanov V. V., LANGER T., Maes L. A Novel Series of [1,2,4]Triazolo[4,3-a]Pyridine Sulfonamides as Potential Antimalarial Agents: In Silico Studies, Synthesis and In Vitro Evaluation // Molecules. 2020. Vol. 25. No. 19. p. 4485.
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TY - JOUR
DO - 10.3390/molecules25194485
UR - https://doi.org/10.3390/molecules25194485
TI - A Novel Series of [1,2,4]Triazolo[4,3-a]Pyridine Sulfonamides as Potential Antimalarial Agents: In Silico Studies, Synthesis and In Vitro Evaluation
T2 - Molecules
AU - Karpina, Veronika R.
AU - Kovalenko, Svitlana S.
AU - Kovalenko, Sergiy M.
AU - Drushlyak, Oleksandr G
AU - Bunyatyan, Natalya D.
AU - Georgiyants, Victoriya A.
AU - Ivanov, Vladimir V
AU - LANGER, Thierry
AU - Maes, Louis
PY - 2020
DA - 2020/09/30
PB - MDPI
SP - 4485
IS - 19
VL - 25
PMID - 33007887
SN - 1420-3049
ER -
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BibTex (до 50 авторов)
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@article{2020_Karpina,
author = {Veronika R. Karpina and Svitlana S. Kovalenko and Sergiy M. Kovalenko and Oleksandr G Drushlyak and Natalya D. Bunyatyan and Victoriya A. Georgiyants and Vladimir V Ivanov and Thierry LANGER and Louis Maes},
title = {A Novel Series of [1,2,4]Triazolo[4,3-a]Pyridine Sulfonamides as Potential Antimalarial Agents: In Silico Studies, Synthesis and In Vitro Evaluation},
journal = {Molecules},
year = {2020},
volume = {25},
publisher = {MDPI},
month = {sep},
url = {https://doi.org/10.3390/molecules25194485},
number = {19},
pages = {4485},
doi = {10.3390/molecules25194485}
}
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MLA
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Karpina, Veronika R., et al. “A Novel Series of [1,2,4]Triazolo[4,3-a]Pyridine Sulfonamides as Potential Antimalarial Agents: In Silico Studies, Synthesis and In Vitro Evaluation.” Molecules, vol. 25, no. 19, Sep. 2020, p. 4485. https://doi.org/10.3390/molecules25194485.