Parveen_2016_J.Photochem.Photobiol.B_161_304

Reference

Title : Potent acetylcholinesterase inhibitors: Synthesis, biological assay and docking study of nitro acridone derivatives - Parveen_2016_J.Photochem.Photobiol.B_161_304
Author(s) : Parveen M , Aslam A , Nami SA , Malla AM , Alam M , Lee DU , Rehman S , Silva PS , Silva MR
Ref : J Photochem Photobiol B , 161 :304 , 2016
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, 1H, 13C 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=0.22muM). 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.

PubMedSearch : Parveen_2016_J.Photochem.Photobiol.B_161_304
PubMedID: 27295412

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Citations formats

Parveen M, Aslam A, Nami SA, Malla AM, Alam M, Lee DU, Rehman S, Silva PS, Silva MR (2016)
Potent acetylcholinesterase inhibitors: Synthesis, biological assay and docking study of nitro acridone derivatives
J Photochem Photobiol B 161 :304

Parveen M, Aslam A, Nami SA, Malla AM, Alam M, Lee DU, Rehman S, Silva PS, Silva MR (2016)
J Photochem Photobiol B 161 :304