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 |
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Format: | Artikel |
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. |
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ISSN: | 1070-4280 1608-3393 |
DOI: | 10.1134/S1070428021120198 |