Anti-HIV and Antimicrobial Activity of 7-Hydrazino-8-hydroxyquinoline-Based Aromatic Hydrazones

Aromatic hydrazones of 7-hydrazino-8-hydroxyquinoline were studied as anti-HIV and antibacterial compounds. A set of the compounds with different aromatic moieties bearing electron-donating and electron-withdrawing substituents has been selected and obtained via the hydrazo coupling and "one-pot" click reaction with aldehydes. The compounds possess activity against both bacterial and fungal targets. Cellular Ku70-inhibiting activity has been found for the series, opening a new class of inhibitors for potential anti-HIV treatment. The compounds display anti-HIV activity in infected cells at submicromolar concentrations. Their low solubility can be overcome by incorporation in water-soluble neutral polyalginate microgels (33% wt load of the compound).

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Journal
International Journal of Molecular Sciences
Published
2025-08-29
DOI
https://doi.org/10.3390/ijms26178402
Primary Topic
Click Chemistry and Applications
Type
article
Field-Weighted Citation Impact
0.00

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article

Anti-HIV and Antimicrobial Activity of 7-Hydrazino-8-hydroxyquinoline-Based Aromatic Hydrazones

С. П. Королев, Vladimir T. Valuev-Elliston, Sergey N. Kochetkov, Anastasia S. Zemskaya et al.
International Journal of Molecular Sciences
Click Chemistry and Applications
article

Anti-HIV and Antimicrobial Activity of 7-Hydrazino-8-hydroxyquinoline-Based Aromatic Hydrazones

С. П. Королев, Vladimir T. Valuev-Elliston, Sergey N. Kochetkov, Anastasia S. Zemskaya, Daria K. Sherman, Lyudmila B. Kalnina, Pavel N. Solyev, Svetlana V. Revtovich, Marina Gottikh, Marat M. Khisamov, Vasiliy V. Spiridonov, Yaroslav V. Kozmenko
article en

Abstract

Aromatic hydrazones of 7-hydrazino-8-hydroxyquinoline were studied as anti-HIV and antibacterial compounds. A set of the compounds with different aromatic moieties bearing electron-donating and electron-withdrawing substituents has been selected and obtained via the hydrazo coupling and "one-pot" click reaction with aldehydes. The compounds possess activity against both bacterial and fungal targets. Cellular Ku70-inhibiting activity has been found for the series, opening a new class of inhibitors for potential anti-HIV treatment. The compounds display anti-HIV activity in infected cells at submicromolar concentrations. Their low solubility can be overcome by incorporation in water-soluble neutral polyalginate microgels (33% wt load of the compound).

International Journal of Molecular SciencesVol. 26(17)
Engelhardt Institute of Molecular Biology (RU), Lomonosov Moscow State University (RU), Gamalei Institute of Epidemiology and Microbiology (RU), D.I. Ivanovsky Institute of Virology Russian Academy of Medical Sciences (RU)
Russian Science Foundation
Openalex Percentile: Top 83%
Click Chemistry and Applications
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Anti-HIV and Antimicrobial Activity of 7-Hydrazino-8-hydroxyquinoline-Based Aromatic Hydrazones — С. П. Королев, Vladimir T. Valuev-Elliston, et al. · International Journal of Molecular Sciences (2025) | TGRS Research Map | TGRS