One-Pot Multicomponent Synthesis, Molecular Docking, and In Vitro Antibacterial Activities of 1-{(Aryl)[(5-methyl-1,3-thiazol-2-yl)amino]methyl}naphthalen-2-ol

A series of new Betti bases, 1-{(aryl)[(5-methyl-1,3-thiazol-2-yl)amino]methyl}naphthalen-2-ols, have been synthesized via one-pot three-component reaction of aromatic aldehydes, 5-methyl-1,3-thiazol-2-amine, and naphthalen-2-ol in glycerol in the presence of silica sulfuric acid (SSA) as a catalyst...

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Veröffentlicht in:Russian journal of organic chemistry 2021-12, Vol.57 (12), p.2024-2030
Hauptverfasser: Lotlikar, O. A., Dandekar, S. N., Ramana, M. M. V., Rathod, S. V.
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Sprache:eng
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Zusammenfassung:A series of new Betti bases, 1-{(aryl)[(5-methyl-1,3-thiazol-2-yl)amino]methyl}naphthalen-2-ols, have been synthesized via one-pot three-component reaction of aromatic aldehydes, 5-methyl-1,3-thiazol-2-amine, and naphthalen-2-ol in glycerol in the presence of silica sulfuric acid (SSA) as a catalyst. The synthesized compounds were evaluated for their in vitro antibacterial activity against S. aureus , B. subtilis , E. coli , and P. aeruginosa using ciprofloxacin as a standard drug. Molecular docking analysis ascertained that the anti­microbial potential of these derivatives is determined by inhibition of DNA gyrase. In silico ADMET analysis of the title compounds was also performed.
ISSN:1070-4280
1608-3393
DOI:10.1134/S1070428021120198