Synthesis and Antimicrobial Action of Ninhydrin, Isatin, and 5-Acetyl-4-Hydroxy-1,3-Thiazine-2,6-Dione Derivatives Against Staphylococcus aureus and Pseudomonas aeruginosa Opportunistic Microflora
A S Zukhairaeva
1, 2
,
A V Velikorodov
1, 2
,
L V Saroyants
2, 3
,
M Yu Yushin
3
,
A V Lutsenko
2, 3
,
E A Shustova
2
3
Leprosy Research Institute, Ministry of Healthcare of the Russian Federation, Astrakhan, Russia
|
Publication type: Journal Article
Publication date: 2022-08-16
scimago Q4
wos Q4
SJR: 0.219
CiteScore: 1.4
Impact factor: 1.0
ISSN: 0091150X, 15739031
Drug Discovery
Pharmacology
Abstract
Series of new derivatives of ninhydrin, isatin, and 4-hydroxy-1,3-thiazine-2,6-dione were synthesized. Their antimicrobial activity against opportunistic microflora of Staphylococcus aureus and Pseudomonas aeruginosa isolated from neurotrophic ulcers of leprosy patients was studied. Antibacterial activity against S. aureus was observed for derivatives of chalcone (MIC 2.31 ± 0.99 and 8.0 ± 2.83 μg/mL), benzofuran (MIC 3.5 ± 1.66 μg/mL), imines (MIC 0.56 ± 0.16 and 3.01 ± 1.68 μg/mL), and indene (MIC 1.38 ± 0.38 μg/mL). Derivatives of imine (MIC 0.25 ± 0.05 and 0.63 ± 0.26 μg/mL) and indene also exhibited pronounced inhibitory effects against P. aeruginosa. Bactericidal effects on both cultures were observed for 5-{(1E)-1-[2-(1-benzothiophen-2-yl)hydrazinylidene]-ethyl}-4-hydroxy-2H-1,3-thiazine-2,6(3H)-dione. An indene derivative with a morpholine fragment showed a pronounced bactericidal effect (MBC 2.3 ± 0.58 μg/mL) on the growth of P. aeruginosa culture.
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Zukhairaeva A. S. et al. Synthesis and Antimicrobial Action of Ninhydrin, Isatin, and 5-Acetyl-4-Hydroxy-1,3-Thiazine-2,6-Dione Derivatives Against Staphylococcus aureus and Pseudomonas aeruginosa Opportunistic Microflora // Pharmaceutical Chemistry Journal. 2022. Vol. 56. No. 5. pp. 597-601.
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Zukhairaeva A. S., Velikorodov A. V., Saroyants L. V., Yushin M. Yu., Lutsenko A. V., Shustova E. A. Synthesis and Antimicrobial Action of Ninhydrin, Isatin, and 5-Acetyl-4-Hydroxy-1,3-Thiazine-2,6-Dione Derivatives Against Staphylococcus aureus and Pseudomonas aeruginosa Opportunistic Microflora // Pharmaceutical Chemistry Journal. 2022. Vol. 56. No. 5. pp. 597-601.
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TY - JOUR
DO - 10.1007/s11094-022-02682-3
UR - https://doi.org/10.1007/s11094-022-02682-3
TI - Synthesis and Antimicrobial Action of Ninhydrin, Isatin, and 5-Acetyl-4-Hydroxy-1,3-Thiazine-2,6-Dione Derivatives Against Staphylococcus aureus and Pseudomonas aeruginosa Opportunistic Microflora
T2 - Pharmaceutical Chemistry Journal
AU - Zukhairaeva, A S
AU - Velikorodov, A V
AU - Saroyants, L V
AU - Yushin, M Yu
AU - Lutsenko, A V
AU - Shustova, E A
PY - 2022
DA - 2022/08/16
PB - Springer Nature
SP - 597-601
IS - 5
VL - 56
SN - 0091-150X
SN - 1573-9031
ER -
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BibTex (up to 50 authors)
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@article{2022_Zukhairaeva,
author = {A S Zukhairaeva and A V Velikorodov and L V Saroyants and M Yu Yushin and A V Lutsenko and E A Shustova},
title = {Synthesis and Antimicrobial Action of Ninhydrin, Isatin, and 5-Acetyl-4-Hydroxy-1,3-Thiazine-2,6-Dione Derivatives Against Staphylococcus aureus and Pseudomonas aeruginosa Opportunistic Microflora},
journal = {Pharmaceutical Chemistry Journal},
year = {2022},
volume = {56},
publisher = {Springer Nature},
month = {aug},
url = {https://doi.org/10.1007/s11094-022-02682-3},
number = {5},
pages = {597--601},
doi = {10.1007/s11094-022-02682-3}
}
Cite this
MLA
Copy
Zukhairaeva, A. S., et al. “Synthesis and Antimicrobial Action of Ninhydrin, Isatin, and 5-Acetyl-4-Hydroxy-1,3-Thiazine-2,6-Dione Derivatives Against Staphylococcus aureus and Pseudomonas aeruginosa Opportunistic Microflora.” Pharmaceutical Chemistry Journal, vol. 56, no. 5, Aug. 2022, pp. 597-601. https://doi.org/10.1007/s11094-022-02682-3.