scholarly journals Synthesis, Antimicrobial Screening, Homology Modeling, and Molecular Docking Studies of a New Series of Schiff Base Derivatives as Prospective Fungal Inhibitor Candidates

Molecules ◽  
2019 ◽  
Vol 24 (18) ◽  
pp. 3250 ◽  
Author(s):  
Yahya Toubi ◽  
Farid Abrigach ◽  
Smaail Radi ◽  
Faiza Souna ◽  
Abdelkader Hakkou ◽  
...  
Keyword(s):  
Schiff Base ◽  
Homology Modeling ◽  
Condensation Reaction ◽  
Docking Studies ◽  
Antifungal Effect ◽  
1H And 13C Nmr ◽  
Schiff Base Derivatives ◽  
Ft Ir ◽  
Antibacterial And Antifungal

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.

Synthesis,Characterization and Evaluation of Biological Activity of Sulfonylhydrazide-Schiff Base" (E)- N’-(2,5-dimethoxybenzalidene) naphthalene-2-sulfonohydrazide"

2020 ◽  
Vol 8 (1) ◽  
pp. 01-11
Author(s):  
Sameer Amereih ◽  
Abd Daraghmeh ◽  
Ismail Warad ◽  
Mohammed Al-Nuri
Keyword(s):  
Schiff Base ◽  
Inhibitory Concentration ◽  
Condensation Reaction ◽  
Gram Negative Bacteria ◽  
Biological Applications ◽  
Bacteriostatic Effect ◽  
1H And 13C Nmr ◽  
13C Nmr Analysis ◽  
Ft Ir

Condensation reaction of naphthalene -2-Sulfonylhydrazide, as starting material with 2,5-dimethoxy benzaldehyde was used to produce (E)-N’-(2,5-dimethoxybenzalidene)naphthalene-2-sulfonohydrazide. The Schiff base product was isolated, purified and then spectrally characterized via UV-Vis, GC/MS, FT-IR, 1H and 13C NMR analysis, where strong evidences confirmed the formation of the desired product. Antimicrobial activity of Schiff base product was evaluated in vitro against several types of bacteria such as: Escherichia coli, Staphylococcus aureus, Pseudomonas aeruginosa, Klebsiella pneumoniae and MRSA by Minimum Inhibitory Concentration (MIC) test using tetracycline (TE) as a standard antibiotic. The tests showed a promising bacteriostatic effect of this compound against gram negative bacteria such as P. aeruginosa and K. pneumoniae, such character is valuable for biological applications.

Synthesis and Evaluation of Anti-Lipase Potential and Molecular Docking of N’-(2-Hydroxy-5-nitrobenzylidene) naphthalene-2-sulfonohydrazide

2020 ◽  
Vol 8 (2) ◽  
pp. 01-11
Author(s):  
Sameer Amereih ◽  
Abd Daraghmeh ◽  
Ismail Warad ◽  
Mohammed Al-Nuri
Keyword(s):  
Schiff Base ◽  
Molecular Docking ◽  
Enzyme Inhibitor ◽  
Condensation Reaction ◽  
Klebsiella Pneumonia ◽  
1H And 13C Nmr ◽  
Lipase Enzyme ◽  
13C Nmr Analysis ◽  
Ft Ir

N’-(2-Hydroxy-5-nitrobenzylidene) naphthalene-2-sulfonohydrazide (SB) was prepared by condensation reaction, of naphthalene-2-sulfonylchloride with 2-Hydroxy-5-nitrobenzaldehyde. The Schiff base product (SB) was isolated, purified and then spectrally characterized via UV-Vis, FT-IR, 1H and 13C NMR analysis, where strong evidences confirmed the formation of the desired product. Pancreatic porcine lipase inhibition of the Schiff base product was evaluated and compared with the reference “Orlistat”. The product was an active as a lipase enzyme inhibitor with IC50 42.65±0.97 mcg/ml. The molecular docking of the compound with porcine pancreatic lipase was investigating, the results of theoretical docking explained the  experimental one since several hydrogen bonds between the Schiff base compound and amino acids in lipase were detected. Antimicrobial activity of SB product was also evaluated in vitro against several types of bacteria such as: Escherichia coli, Staphylococcus aureus, Pseudomonas aeruginosa, Klebsiella pneumonia and MRSA by Minimum Inhibitory Concentration (MIC) test using tetracycline (TE) as a standard antibiotic. Results showed a bacteriostatic effect of this compound against bacteria such as MRSA, P. aeruginosa and K. pneumoniae

Synthesis,Characterization and Evaluation of Biological Activity of Sulfonylhydrazide-Schiff Base" (E)- N’-(2,5-dimethoxybenzalidene) naphthalene-2-sulfonohydrazide"

2020 ◽  
Vol 8 (1) ◽  
pp. 01-11
Author(s):  
Sameer Amereih ◽  
Abd Daraghmeh ◽  
Ismail Warad ◽  
Mohammed Al-Nuri
Keyword(s):  
Schiff Base ◽  
Inhibitory Concentration ◽  
Condensation Reaction ◽  
Gram Negative Bacteria ◽  
Biological Applications ◽  
Bacteriostatic Effect ◽  
1H And 13C Nmr ◽  
13C Nmr Analysis ◽  
Ft Ir

Condensation reaction of naphthalene -2-Sulfonylhydrazide, as starting material with 2,5-dimethoxy benzaldehyde was used to produce (E)-N’-(2,5-dimethoxybenzalidene)naphthalene-2-sulfonohydrazide. The Schiff base product was isolated, purified and then spectrally characterized via UV-Vis, GC/MS, FT-IR, 1H and 13C NMR analysis, where strong evidences confirmed the formation of the desired product. Antimicrobial activity of Schiff base product was evaluated in vitro against several types of bacteria such as: Escherichia coli, Staphylococcus aureus, Pseudomonas aeruginosa, Klebsiella pneumoniae and MRSA by Minimum Inhibitory Concentration (MIC) test using tetracycline (TE) as a standard antibiotic. The tests showed a promising bacteriostatic effect of this compound against gram negative bacteria such as P. aeruginosa and K. pneumoniae, such character is valuable for biological applications.

Synthesis and Evaluation of Anti-Lipase Potential and Molecular Docking of N’-(2-Hydroxy-5-nitrobenzylidene) naphthalene-2-sulfonohydrazide

2020 ◽  
Vol 8 (2) ◽  
pp. 01-11
Author(s):  
Sameer Amereih ◽  
Abd Daraghmeh ◽  
Ismail Warad ◽  
Mohammed Al-Nuri
Keyword(s):  
Schiff Base ◽  
Molecular Docking ◽  
Enzyme Inhibitor ◽  
Condensation Reaction ◽  
Klebsiella Pneumonia ◽  
1H And 13C Nmr ◽  
Lipase Enzyme ◽  
13C Nmr Analysis ◽  
Ft Ir

N’-(2-Hydroxy-5-nitrobenzylidene) naphthalene-2-sulfonohydrazide (SB) was prepared by condensation reaction, of naphthalene-2-sulfonylchloride with 2-Hydroxy-5-nitrobenzaldehyde. The Schiff base product (SB) was isolated, purified and then spectrally characterized via UV-Vis, FT-IR, 1H and 13C NMR analysis, where strong evidences confirmed the formation of the desired product. Pancreatic porcine lipase inhibition of the Schiff base product was evaluated and compared with the reference “Orlistat”. The product was an active as a lipase enzyme inhibitor with IC50 42.65±0.97 mcg/ml. The molecular docking of the compound with porcine pancreatic lipase was investigating, the results of theoretical docking explained the  experimental one since several hydrogen bonds between the Schiff base compound and amino acids in lipase were detected. Antimicrobial activity of SB product was also evaluated in vitro against several types of bacteria such as: Escherichia coli, Staphylococcus aureus, Pseudomonas aeruginosa, Klebsiella pneumonia and MRSA by Minimum Inhibitory Concentration (MIC) test using tetracycline (TE) as a standard antibiotic. Results showed a bacteriostatic effect of this compound against bacteria such as MRSA, P. aeruginosa and K. pneumoniae

scholarly journals Synthesis and Characterization of New Amino Acid-Schiff Bases and Studies their Effects on the Activity of ACP, PAP and NPA Enzymes (In Vitro)

2012 ◽  
Vol 9 (2) ◽  
pp. 962-969 ◽  
Author(s):  
Zahraa Salim M. Al-Garawi ◽  
Ivan Hameed R. Tomi ◽  
Ali Hussein R. Al-Daraji
Keyword(s):  
Schiff Base ◽  
Condensation Reaction ◽  
Synthesis And Characterization ◽  
Activation Effect ◽  
Inhibition Effect ◽  
H Nmr ◽  
Ft Ir ◽  
High Concentrations

In this study, two new Schiff base compounds derived from the condensation reaction ofL-glycine andL-tryptophan with 4-methylbenzal-dehyde have been synthesized. The Schiff base compounds were characterized by FT-IR, UV and1H NMR spectroscopy. Their effects on the activity of total (ACP), prostatic (PAP) and non prostatic (NPA) acid phosphatase enzymes were studied. The Schiff base derived fromL-glycine (A) demonstrated inhibition effect on the ACP and NPA activities and activation effect on PAP activity. The Schiff base derived fromL-tryptophan (B) demonstrated semi fixed inhibition effects on the ACP and NPA activities at high concentrations (5.5×10-2, 5.5×10-3and 5.5×10-4M) and activator effect at low concentration (5.5×10-5M) while it was exhibits as activator on PAP activity.

scholarly journals Synthesis of disulphide-Schiff base derivatives and investigations of in vitro antimicrobial activities against some human pathogens

2017 ◽  
Vol 1 (3) ◽  
pp. 230-234 ◽  
Author(s):  
Sefa Durmuş ◽  
Aslıhan Dalmaz ◽  
Görkem Dülger ◽  
Duygu Bircan Kadıoğlu
Keyword(s):  
Schiff Base ◽  
Schiff Bases ◽  
Antimicrobial Activities ◽  
Diffusion Method ◽  
Control Group ◽  
Human Pathogens ◽  
Antibacterial And Antifungal Activities ◽  
Schiff Base Derivatives ◽  
Antibacterial And Antifungal

Abstract Thio-Schiff bases are becoming increasingly widespread in various branches such as the preparation of certain medicines, cosmetic products, and polymer production. In particular, the presence of antibacterial, antifungal, antiviral, antitumor and antimalarial properties of Schiff bases containing sulfur in the structure has made these compounds attractive in different disciplines. In this study, different derivatives of dimeric disulfide-Schiff bases have been synthesized. The antibacterial and antifungal activities of the synthesized these compounds were investigated in vitro against some human pathogens (Acinetobacter baumannii, Escherichia coli, Klebsiella pneumoniae, Staphylococcus aureus and Candida albicans, C. tropicalis, C. guilliermondii and C. glabrata). Test microorganisms were isolated from the patients appyling to Medical Faculty Hospital of Duzce University were used. Diffusion method was used to determine the antimicrobial activities of the compounds.standard antibacterial (Cefotaxime, Amoxicillin/clavulanicacid) and antifungal (Posaconazole) antibiotics were used as the control group and the results were compared. The result indicated that antimicrobial activity of Disulphide-Schiff Base Derivatives exhibited less activity against bacteria as compared to AMC30 (Amoxicillin/clavulanicacid), but highly effective against bacteria as compared to CTX30 (Cefotaxime). In addition, the compounds exhibited less activity against yeast.

scholarly journals Synthesis and Structural Characterization of (E)-4-[(2-Hydroxy-3-methoxybenzylidene)amino]butanoic Acid and Its Novel Cu(II) Complex

Molbank ◽  
10.3390/m1179 ◽  
2021 ◽  
Vol 2021 (1) ◽  
pp. M1179
Author(s):  
Eleftherios Halevas ◽  
Antonios Hatzidimitriou ◽  
Barbara Mavroidi ◽  
Marina Sagnou ◽  
Maria Pelecanou ◽  
...  
Keyword(s):  
Schiff Base ◽  
Gamma Aminobutyric Acid ◽  
X Ray Diffraction ◽  
Reaction Conditions ◽  
Polymeric Compound ◽  
Bridging Ligands ◽  
1H And 13C Nmr ◽  
One Dimensional ◽  
Ft Ir

A novel Cu(II) complex based on the Schiff base obtained by the condensation of ortho-vanillin with gamma-aminobutyric acid was synthesized. The compounds are physico-chemically characterized by elemental analysis, HR-ESI-MS, FT-IR, and UV-Vis. The complex and the Schiff base ligand are further structurally identified by single crystal X-ray diffraction and 1H and 13C-NMR, respectively. The results suggest that the Schiff base are synthesized in excellent yield under mild reaction conditions in the presence of glacial acetic acid and the crystal structure of its Cu(II) complex reflects an one-dimensional polymeric compound. The molecular structure of the complex consists of a Cu(II) ion bound to two singly deprotonated Schiff base bridging ligands that form a CuN2O4 chelation environment, and a coordination sphere with a disordered octahedral geometry.

Synthesis, in vitro and in vivo antitumor activity of symmetrical bis-Schiff base derivatives of isatin

2014 ◽  
Vol 74 ◽  
pp. 742-750 ◽  
Author(s):  
Chengyuan Liang ◽  
Juan Xia ◽  
Dong Lei ◽  
Xiang Li ◽  
Qizheng Yao ◽  
...  
Keyword(s):  
Schiff Base ◽  
Antitumor Activity ◽  
Schiff Base Derivatives ◽  
In Vivo Antitumor Activity ◽  
Derivatives Of

scholarly journals Synthesis, in vitro and in silico Studies of Naphthalene Pyrazoline Prop-2-en-1-one Derivatives

2020 ◽  
Vol 32 (8) ◽  
pp. 1849-1856
Author(s):  
B. Prabha ◽  
C. Raja ◽  
S. Nathiya ◽  
M.R. Ezhilarasi
Keyword(s):  
Binding Affinity ◽  
Addition Reaction ◽  
Condensation Reaction ◽  
Docking Studies ◽  
High Drug ◽  
In Silico Studies ◽  
Drug Score ◽  
The Michael Addition ◽  
High Inhibition

The synthesized new naphthalene pyrazoline prop-2-en-1-one derivatives (NDPP 1-8) were obtained by the Michael addition reaction of ethyl propanoate, hydrazine hydrate with NPD as a multicomponent scaffold. (E)-1-(naphthalen-3-yl)-3-phenylprop-2-en-1-one (NPD) was formed from 2-acetyl naphthalene and substituted aldehyde via Claisen-Schmidt condensation reaction. The NDPP skeleton structures were confirmed by infrared, 1H & 13C NMR spectral data and elemental analysis. The structure of NDPP compounds was subjected to molecular docking and ADME studies. The result of ADME prediction, compound NDPP 2, which contains electron withdrawing -Cl group has high drug-likeness value 4.21 than the compounds NDPP 4 and 7 which had electron donating CH3 and OCH3 group shows the drug-likeness value 2.62. The NDPP 2 also has high drug score 0.63 than NDPP 4 and NDPP 7 have drug score 0.60 and 0.69, respectively. Docking studies shows that compound NDPP 5 which also contain electron withdrawing NO2 group has good binding affinity value -8.8 Kcal/mol were docked with 1UAG protein. These compounds showed good drug-likeness value 2.25 and drug score 0.65. in vitro Studies have a high inhibition value for the same NO2 substituted derivative. All the compounds have higher binding affinity value than standards binding affinity value.

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