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IJMS, Vol. 25, Pages 11130: Biological Activity Evaluation of Phenolic Isatin-3-Hydrazones Containing a Quaternary Ammonium Center of Various Structures
International Journal of Molecular Sciences doi: 10.3390/ijms252011130
Authors: Margarita Neganova Yulia Aleksandrova Alexandra Voloshina Anna Lyubina Nurbol Appazov Sholpan Yespenbetova Zulfiia Valiullina Aleksandr Samorodov Sergey Bukharov Elmira Gibadullina Anipa Tapalova Andrei Bogdanov
A series of new isatin-3-hydrazones bearing different ammonium fragments was synthesized by a simple and easy work-up reaction of Girard’s reagents analogs with 1-(3,5-di-tert-butyl-4-hydroxybenzyl)isatin. All derivatives have been shown to have antioxidant properties. In terms of bactericidal activity against gram-positive bacteria, including methicillin-resistant strains of Staphylococcus aureus, the best compounds are 3a, 3e, and 3m, bearing octyl, acetal, and brucine ammonium centers, respectively. In addition, brucine and quinine derivatives 3l, and 3j exhibit platelet antiaggregation activity at the level of acetylsalicylic acid, and this series of isatin derivatives does not adversely affect the hemostasis system as a whole. Thus, all the obtained results can lay the groundwork for future pharmaceutical developments for the creation of effective antibacterial drugs with reduced systemic toxicity due to the presence of antioxidant properties.
