Potent acetylcholinesterase inhibitors: Synthesis, biological assay and docking study of nitro acridone derivatives.
J Photochem Photobiol B
; 161: 304-11, 2016 Aug.
Article
em En
| MEDLINE
| ID: mdl-27295412
ABSTRACT
The reaction of o-halobenzoic acid with aniline derivatives and their subsequent cyclization reaction yielded the acridone derivatives. The series of nitro acridone derivatives were prepared by Ullmann condensation in presence of copper as catalyst and were characterized by FTIR, (1)H, (13)C NMR and mass spectra. The structure of 5-nitro-(2-phenyl amino) benzoic acid (4) was confirmed by X-ray crystallography and was found to crystallize in P21/c space group. The in vitro efficacy of the compounds for their acetylcholinesterase (AChE) and antimicrobial inhibitory activities have been evaluated against the standard drugs Ampicillin and Gentamicin against Gram positive and Gram negative bacteria. 1,7-Dinitroacridone was found to be the most potent AChE inhibitor (IC50=0.22µM). Moreover, the compounds have been screened for their antioxidant activity using the DPPH assay. Also, docking study results were found to be in good agreement with the results obtained through in vitro experiments. The docking study further predicted possible binding conformation.
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Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Inibidores da Colinesterase
/
Acridonas
Idioma:
En
Revista:
J Photochem Photobiol B
Assunto da revista:
BIOLOGIA
Ano de publicação:
2016
Tipo de documento:
Article