Journal of Enzyme Inhibition and Medicinal Chemistry, Mar 25, 2014
A simple and efficient method for the synthesis of highly diverse pyrano[2,3-c]pyridazines was ac... more A simple and efficient method for the synthesis of highly diverse pyrano[2,3-c]pyridazines was achieved by a one pot multicomponent reaction using piperidine as the organocatalyst. The synthesis of a series of heterocyclic derivatives with varying functionality (e.g. thiazine, tetrazole and pyrimidine) incorporating the pyrano[2,3-c]pyridazine moiety were achieved via reaction of 2a-e with different reagents. The structures of the synthesized derivatives were elucidated by FTIR, MS, (1)H and (13)C NMR spectroscopy. A number of the newly synthesized targeted compounds 2b-e, 3a-c and 4a-c were evaluated for their in vitro antibacterial activity and were compared with chloramphenicol and nystatin as broad spectrum reference standard antibiotics. Tests were carried out against Staphylococcus aureus (MTCC3160) and Enterococcusi fecalis as Gram-positive bacteria, and Escherichia coli (MTCC1652) and Klebsiella pneumonia as Gram-negative bacteria. Antifungal potential against Candida albicans, and Aspergillus albicans strains were also evaluated. The results revealed that compounds 3a and 3c showed strong significant activity relative to the reference against these bacterial and fungal strains.
International Journal of Biological Macromolecules, Sep 1, 2020
Synthesis of new hydrazinocurcumin derivative 4-((E)-2-(1-(4-Methoxy benzyl)-6-p-tolylpyridazin-3... more Synthesis of new hydrazinocurcumin derivative 4-((E)-2-(1-(4-Methoxy benzyl)-6-p-tolylpyridazin-3-yl)-3-((E)-4-hydroxy-3-methoxystyryl)-1H-pyrazol-5-yl)vinyl)-2-methoxyphenol (HCUR) through the reaction of curcumin (CUR) with 1- (4-(2-Methoxybenzyl)-6-p-tolylpyridazin-3-yl)hydrazine(VII). Nanoparticles formulations of (HCUR) loaded chitosan (CS), ZnO, Au, CS-ZnO and CS-Au NPs, via self-assembling process were developed to give CS-HCUR NPs, ZnO-HCUR NPs, Au-HCUR NPs, CS-ZnO-HCUR NPs and CS-Au-HCUR NPs. Chemical structures of (HCUR) and (HCUR) loaded nanoparticles formulations were characterized by UV-Vis, FTIR, Mass Spectrum, Elemental Analysis, 1HNMR, 13CNMR, TGA, DSC, SEM and TEM. The particle size of the nanoformulations ranged from 16.8 to 59.6 nm. NPs formulations were used as delivery system to sustain controlled drug delivery. Drug release profiles and cytotoxicity of NPs formulations against HCT-116 (colon carcinoma) and HepG-2 (hepatocellular cancer) cell lines were investigated. Drug release studies showed that by decreasing the pH value of release medium from 7.4 to 5.4 increased the release rate of (HCUR) from the NPs formulations. Cell viability study proved that NPs formulations revealed higher activity against HCT- 116 cell than (CUR) especially CS-HCUR NPs which displayed the most active with cell viability 1.80%. Moreover, ZnO-HCUR NPs expressed as the highest cytotoxic effect against HepG-2 cell with cell viability 0.98%.
In this paper, new biodegradable hydrogels were prepared, characterized and evaluated for metal i... more In this paper, new biodegradable hydrogels were prepared, characterized and evaluated for metal ions absorption capacity from aqueous systems. The hydrogels are based on reaction of chitosan with polyvinyl alcohol, chitosan and polyvinyl alcohol with glutaraldehyde, N,N′-biisomaleimide, and N,N′-biisophthalimide under different reaction conditions to give the corresponding hydrogels P-C(I), P-C-G(II), P-C-B (III), and P-C-P(IV). The new hydrogels were characterized by FTIR spectroscopy, thermal stability, morphology, crystallography, solubility and swelling ratio. This preliminary investigation of the metal ion entrapment efficiency of the hydrogels showed that chitosan–polyvinyl alcohol–N,N′-biisophthalimide [P-C-P(IV)] hydrogel recovered Cu2+ ions with efficiencies reaching 52.5%, and for Co2+ ions 72.5% from aqueous solution systems.
Environment friendly modified chitosan hydrogels for metal ions absorption from aqueous systems w... more Environment friendly modified chitosan hydrogels for metal ions absorption from aqueous systems were designed using simple technology. Chitosan was modified with [N,N′-bi-α-azidosuccinimide and N-phthalimido-α-azide succinimide] under different reaction conditions to prepare new hydrogels with high metal ion absorption efficiency. The hydrogels were characterized by FTIR, thermal stability, crystallography, solubility and swelling capacity. Promising results were obtained from this preliminary study
European journal of medicinal chemistry, May 1, 2009
A general method for the preparation of new hydrazones is reported. The 1-[4-(2-methoxybenzyl)-6-... more A general method for the preparation of new hydrazones is reported. The 1-[4-(2-methoxybenzyl)-6-aryl pyridazin-3(2H)-ylidene] hydrazines or their tautomeric structures (1(a-d)) were condensed with different aldehydes, dialdehydes, ketones, alpha-dicarbonyl compounds and simple carbohydrates to afford the hydrazones and dihydrazones (2(a-d)), (3(a-d)), (4(a-d)), (5(a-d)), (6(d)), (7(c)), (8(a-d)), (9(a-d)), (10(a-d)), (11(a-d)), (12(a,c,d)), (13(a-d)), (14(a-d)), (15(a-d)), (16(a-d)) and (17(a-d)). The structures of all synthesized compounds were confirmed from microanalytical and spectral data. Some of the products were screened for their antimicrobial activity against Staphylococcus aureus and Streptococcus faecalis, Escherichia coli and Pseudomonas aeruginosa. The hydrazone derivative 15(d) (1-[4-(2-methoxybenzyl)-6-methylphenyl pyridazin-3(2H)-ylidene]-2-(2-carboxydiphenyl methyl) hydrazine) showed the highest biological activity.
A new series compounds of quinoline derivatives were synthesized by reaction of 3-(carboxymethyl)... more A new series compounds of quinoline derivatives were synthesized by reaction of 3-(carboxymethyl)-2-arylquinoline-4-carboxylic acids 1a, 1b, 1c with different nucleophiles. The structures of the new compounds were elucidated on the basis of FTIR, 1H-NMR, 13C-NMR spectral data, GC/MS, and chemical analysis. Investigation of antimicrobial activity of all new compounds was evaluated using a broth dilution technique in terms of minimal inhibitory concentration count against four pathogenic bacteria and two pathogenic fungi. Most of the new compounds were significantly active against bacteria and fungi.
Preparation and properties of chitosan modified with heterocycles in absence or presence of glute... more Preparation and properties of chitosan modified with heterocycles in absence or presence of gluteraldehyde as a cross linker is described. New modified chitosan–heterocyclic hydrogels were prepared from chitosan and heterocyclic compounds such as N,N′-biisomaleimide, N,N′-biisophthalimide, and N,N′-phthalimidomaleimide via a crosslinking reaction. The new hydrogels chemical structure was characterized by spectral analysis (IR), X-ray diffraction, thermal gravimetric analysis (TGA), solubility, and swellability in water and different organic solvents. Evaluation of the efficiency of the new hydrogels to uptake copper and cobalt ions from aqueous systems was carried out and promising results were obtained.
Journal of Enzyme Inhibition and Medicinal Chemistry, Nov 19, 2012
An efficient and simple microwave assisted synthesis of sulfonamide derivatives incorporating the... more An efficient and simple microwave assisted synthesis of sulfonamide derivatives incorporating the pyridazine moiety has been developed. These sulfonamides were used for the preparation of new heterocyclic compounds via reaction with different reagents using a microwave irradiation technique. The structures of the newly synthesized compounds were confirmed on the basis of FTIR, (1)H and (13)C-NMR, mass spectral techniques and elemental analyses. Some of the new synthesized compounds were assayed for their in vitro antibacterial activity against Gram-positive bacteria, Staphylococcus aureus and Staphylococcus epidermidis, Gram-negative bacteria, Escherichia coli and Klebsiella pneumonia and antifungal activity against Aspergillus fumigatus and Candida albicans. Most of the new compounds showed significant antibacterial and antifungal activity.
Journal of Enzyme Inhibition and Medicinal Chemistry, Mar 25, 2014
A simple and efficient method for the synthesis of highly diverse pyrano[2,3-c]pyridazines was ac... more A simple and efficient method for the synthesis of highly diverse pyrano[2,3-c]pyridazines was achieved by a one pot multicomponent reaction using piperidine as the organocatalyst. The synthesis of a series of heterocyclic derivatives with varying functionality (e.g. thiazine, tetrazole and pyrimidine) incorporating the pyrano[2,3-c]pyridazine moiety were achieved via reaction of 2a-e with different reagents. The structures of the synthesized derivatives were elucidated by FTIR, MS, (1)H and (13)C NMR spectroscopy. A number of the newly synthesized targeted compounds 2b-e, 3a-c and 4a-c were evaluated for their in vitro antibacterial activity and were compared with chloramphenicol and nystatin as broad spectrum reference standard antibiotics. Tests were carried out against Staphylococcus aureus (MTCC3160) and Enterococcusi fecalis as Gram-positive bacteria, and Escherichia coli (MTCC1652) and Klebsiella pneumonia as Gram-negative bacteria. Antifungal potential against Candida albicans, and Aspergillus albicans strains were also evaluated. The results revealed that compounds 3a and 3c showed strong significant activity relative to the reference against these bacterial and fungal strains.
International Journal of Biological Macromolecules, Sep 1, 2020
Synthesis of new hydrazinocurcumin derivative 4-((E)-2-(1-(4-Methoxy benzyl)-6-p-tolylpyridazin-3... more Synthesis of new hydrazinocurcumin derivative 4-((E)-2-(1-(4-Methoxy benzyl)-6-p-tolylpyridazin-3-yl)-3-((E)-4-hydroxy-3-methoxystyryl)-1H-pyrazol-5-yl)vinyl)-2-methoxyphenol (HCUR) through the reaction of curcumin (CUR) with 1- (4-(2-Methoxybenzyl)-6-p-tolylpyridazin-3-yl)hydrazine(VII). Nanoparticles formulations of (HCUR) loaded chitosan (CS), ZnO, Au, CS-ZnO and CS-Au NPs, via self-assembling process were developed to give CS-HCUR NPs, ZnO-HCUR NPs, Au-HCUR NPs, CS-ZnO-HCUR NPs and CS-Au-HCUR NPs. Chemical structures of (HCUR) and (HCUR) loaded nanoparticles formulations were characterized by UV-Vis, FTIR, Mass Spectrum, Elemental Analysis, 1HNMR, 13CNMR, TGA, DSC, SEM and TEM. The particle size of the nanoformulations ranged from 16.8 to 59.6 nm. NPs formulations were used as delivery system to sustain controlled drug delivery. Drug release profiles and cytotoxicity of NPs formulations against HCT-116 (colon carcinoma) and HepG-2 (hepatocellular cancer) cell lines were investigated. Drug release studies showed that by decreasing the pH value of release medium from 7.4 to 5.4 increased the release rate of (HCUR) from the NPs formulations. Cell viability study proved that NPs formulations revealed higher activity against HCT- 116 cell than (CUR) especially CS-HCUR NPs which displayed the most active with cell viability 1.80%. Moreover, ZnO-HCUR NPs expressed as the highest cytotoxic effect against HepG-2 cell with cell viability 0.98%.
In this paper, new biodegradable hydrogels were prepared, characterized and evaluated for metal i... more In this paper, new biodegradable hydrogels were prepared, characterized and evaluated for metal ions absorption capacity from aqueous systems. The hydrogels are based on reaction of chitosan with polyvinyl alcohol, chitosan and polyvinyl alcohol with glutaraldehyde, N,N′-biisomaleimide, and N,N′-biisophthalimide under different reaction conditions to give the corresponding hydrogels P-C(I), P-C-G(II), P-C-B (III), and P-C-P(IV). The new hydrogels were characterized by FTIR spectroscopy, thermal stability, morphology, crystallography, solubility and swelling ratio. This preliminary investigation of the metal ion entrapment efficiency of the hydrogels showed that chitosan–polyvinyl alcohol–N,N′-biisophthalimide [P-C-P(IV)] hydrogel recovered Cu2+ ions with efficiencies reaching 52.5%, and for Co2+ ions 72.5% from aqueous solution systems.
Environment friendly modified chitosan hydrogels for metal ions absorption from aqueous systems w... more Environment friendly modified chitosan hydrogels for metal ions absorption from aqueous systems were designed using simple technology. Chitosan was modified with [N,N′-bi-α-azidosuccinimide and N-phthalimido-α-azide succinimide] under different reaction conditions to prepare new hydrogels with high metal ion absorption efficiency. The hydrogels were characterized by FTIR, thermal stability, crystallography, solubility and swelling capacity. Promising results were obtained from this preliminary study
European journal of medicinal chemistry, May 1, 2009
A general method for the preparation of new hydrazones is reported. The 1-[4-(2-methoxybenzyl)-6-... more A general method for the preparation of new hydrazones is reported. The 1-[4-(2-methoxybenzyl)-6-aryl pyridazin-3(2H)-ylidene] hydrazines or their tautomeric structures (1(a-d)) were condensed with different aldehydes, dialdehydes, ketones, alpha-dicarbonyl compounds and simple carbohydrates to afford the hydrazones and dihydrazones (2(a-d)), (3(a-d)), (4(a-d)), (5(a-d)), (6(d)), (7(c)), (8(a-d)), (9(a-d)), (10(a-d)), (11(a-d)), (12(a,c,d)), (13(a-d)), (14(a-d)), (15(a-d)), (16(a-d)) and (17(a-d)). The structures of all synthesized compounds were confirmed from microanalytical and spectral data. Some of the products were screened for their antimicrobial activity against Staphylococcus aureus and Streptococcus faecalis, Escherichia coli and Pseudomonas aeruginosa. The hydrazone derivative 15(d) (1-[4-(2-methoxybenzyl)-6-methylphenyl pyridazin-3(2H)-ylidene]-2-(2-carboxydiphenyl methyl) hydrazine) showed the highest biological activity.
A new series compounds of quinoline derivatives were synthesized by reaction of 3-(carboxymethyl)... more A new series compounds of quinoline derivatives were synthesized by reaction of 3-(carboxymethyl)-2-arylquinoline-4-carboxylic acids 1a, 1b, 1c with different nucleophiles. The structures of the new compounds were elucidated on the basis of FTIR, 1H-NMR, 13C-NMR spectral data, GC/MS, and chemical analysis. Investigation of antimicrobial activity of all new compounds was evaluated using a broth dilution technique in terms of minimal inhibitory concentration count against four pathogenic bacteria and two pathogenic fungi. Most of the new compounds were significantly active against bacteria and fungi.
Preparation and properties of chitosan modified with heterocycles in absence or presence of glute... more Preparation and properties of chitosan modified with heterocycles in absence or presence of gluteraldehyde as a cross linker is described. New modified chitosan–heterocyclic hydrogels were prepared from chitosan and heterocyclic compounds such as N,N′-biisomaleimide, N,N′-biisophthalimide, and N,N′-phthalimidomaleimide via a crosslinking reaction. The new hydrogels chemical structure was characterized by spectral analysis (IR), X-ray diffraction, thermal gravimetric analysis (TGA), solubility, and swellability in water and different organic solvents. Evaluation of the efficiency of the new hydrogels to uptake copper and cobalt ions from aqueous systems was carried out and promising results were obtained.
Journal of Enzyme Inhibition and Medicinal Chemistry, Nov 19, 2012
An efficient and simple microwave assisted synthesis of sulfonamide derivatives incorporating the... more An efficient and simple microwave assisted synthesis of sulfonamide derivatives incorporating the pyridazine moiety has been developed. These sulfonamides were used for the preparation of new heterocyclic compounds via reaction with different reagents using a microwave irradiation technique. The structures of the newly synthesized compounds were confirmed on the basis of FTIR, (1)H and (13)C-NMR, mass spectral techniques and elemental analyses. Some of the new synthesized compounds were assayed for their in vitro antibacterial activity against Gram-positive bacteria, Staphylococcus aureus and Staphylococcus epidermidis, Gram-negative bacteria, Escherichia coli and Klebsiella pneumonia and antifungal activity against Aspergillus fumigatus and Candida albicans. Most of the new compounds showed significant antibacterial and antifungal activity.
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