scholarly journals Synthesis of novel Schiff base derivatives of tacrine and investigation of their acetylcholinesterase inhibition potency

2019 ◽  
Vol 38 (1) ◽  
pp. 75 ◽  
Author(s):  
Elif Koyuncu ◽  
Ahmet Yaşar ◽  
Fatma Arslan ◽  
Nurşen Sari

Investigation of acetylcholinesterase (AChE) inhibition potency of some new Schiff base derivatives of tacrine (9-amino-1,2,3,4-tetrahydroacridine) was reported in this paper. Novel Schiff base derivatives of tacrine (3a–g) have been synthesized, and they have been characterized by several methods (FT-IR, 1H-NMR, 13C-NMR, etc.). Then, inhibition effects on AChE by the synthesized compounds have been investigated by the spectrophotometric Ellman method. IC50, Ki, KM and Vmax values and inhibition types have been determined. It was seen that all compounds had the property of a water-soluble reversible AChE inhibitor. Structure 3a was found to be the most potent inhibitor, with the IC50 value of 22.1 ± 1.11  nM (tacrine's IC50 value was calculated as 34.1 nM).

2009 ◽  
Vol 6 (4) ◽  
pp. 1205-1210 ◽  
Author(s):  
J. J. Vora ◽  
S. B. Vasava ◽  
K. C. Parmar ◽  
S. K. Chauhan ◽  
S. S. Sharma

Schiff base derivatives ofN-{(1E)-[3-(mono or di-substituted aryl)-1-phenyl-1H-pyrazol-4-yl]methylene{-4-methylpyridin-2-amine were synthesized by the acid catalyzed condensation of 3-(mono- or di- substituted aryl)-1-phenyl-1H-pyrazole-4-carbaldehyde derivatives with 4-methylpyridin-2-amine. Schiff base derivatives were characterized by FT-IR,1H-NMR, Mass spectral analysis and elemental analysis. All the synthesized compounds have been screened for their antimicrobial activities by using broth dilution method.


2014 ◽  
Vol 74 ◽  
pp. 742-750 ◽  
Author(s):  
Chengyuan Liang ◽  
Juan Xia ◽  
Dong Lei ◽  
Xiang Li ◽  
Qizheng Yao ◽  
...  

2009 ◽  
Vol 2009 (23) ◽  
pp. 3467-3474 ◽  
Author(s):  
Oxana Kotova ◽  
Sergey Semenov ◽  
Svetlana Eliseeva ◽  
Sergey Troyanov ◽  
Konstantin Lyssenko ◽  
...  

2015 ◽  
Vol 45 (4) ◽  
pp. 193-201 ◽  
Author(s):  
Manpreet Kaur ◽  
Jerry P. Jasinski ◽  
Brian J. Anderson ◽  
Hemmige S. Yathirajan ◽  
K. Byrappa

Molecules ◽  
2019 ◽  
Vol 24 (18) ◽  
pp. 3250 ◽  
Author(s):  
Yahya Toubi ◽  
Farid Abrigach ◽  
Smaail Radi ◽  
Faiza Souna ◽  
Abdelkader Hakkou ◽  
...  

Twelve new Schiff base derivatives have been prepared by the condensation reaction of different amino substituted compounds (aniline, pyridin-2-amine, o-toluidine, 2-nitrobenzenamine, 4-aminophenol, and 3-aminopropanol) and substituted aldehydes such as nicotinaldehyde, o,m,p-nitrobenzaldehyde, and picolinaldehyde in ethanol using acetic acid as a catalyst. The envisaged structures of the all the synthesized ligands have been confirmed on the basis of their spectral analysis FT-IR, mass spectroscopy, 1H- and 13C-NMR. In vitro screening of their antibacterial and antifungal potential against Escherichia coli bacterium and Fusarium oxysporum f.sp albedinis (F.o.a) fungus, respectively, revealed that all the ligands showed no significant antibacterial activity, whereas most of them displayed good antifungal activity. Homology modeling and docking analysis were performed to explain the antifungal effect of the most and least active compound against two F.o.a fungus proteins.


1985 ◽  
Vol 98 (1) ◽  
pp. 19-23 ◽  
Author(s):  
S.C. Tripathi ◽  
S.C. Srivastava ◽  
A.K. Shrimal ◽  
O.P. Singh

1975 ◽  
Vol 106 (1) ◽  
pp. 261-270 ◽  
Author(s):  
S. K. Agarwal ◽  
Jai P. Tandon

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