Synthesis and anti-inflammatory activity of novel (substituted)benzylidene acetone oxime ether derivatives: Molecular modeling study

El‐Gamal, Mohammed I.; Bayomi, Said M.; El‐Ashry, Saadia M.; Said, Sameh M.; Abdel‐Aziz, Alaa A.‐M.; Abdel-Aziz, Naglaa I.

doi:10.1016/j.ejmech.2009.12.041

Cited by 53 publications

(21 citation statements)

References 17 publications

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“…Cyclooxygenase (COX) is an enzyme has two isoforms as COX‐1 and COX‐2 . It is known that these isoforms used as selective inhibitors for development of drugs which would be beneficial in the treatment of inflammation (COX‐1 and COX‐2) and pain (COX‐2) . In this work, COX‐1(PDB: 1PRH, PDB: 4O1Z) and COX‐2 (PDB: 4COX, PDB: 3NTB) enzymes was used for the molecular docking study to understand the binding interaction of piperine in the active site of cyclooxygenases.…”

Section: Resultsmentioning

confidence: 99%

Piperine Nanoparticles for Topical Application: Preparation, Characterization,In vitroandIn silicoEvaluation

Budama‐Kilinc

2019

ChemistrySelect

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In this study, piperine was investigated as a drug molecule due to its analgesic and anti‐inflammatory properties. Piperine was encapsulated with poly(lactic‐co‐glycolic acid) (PLGA) in order to increase drug bioavailability for topical applications. Characterization of piperine PLGA nanoparticles (NPs) were performed with spectroscopic and imaging methods. It was found that the piperine PLGA NPs were successfully prepared according to the analyses. The encapsulation efficiency and loading capacity of the piperine were calculated as 99% and 3%, respectively. In vitro release study was also performed. Besides, it was shown that piperine had no mutagenic effect. Finally, molecular docking simulation was performed by using the AutoDock Vina program to identify the interaction between piperine and COX‐1 and COX‐2 enzymes. The aim of this study is to contribute to the design of plant derived nano‐formulations for local anti‐inflammation and pain treatment with better skin penetration.

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Section: Resultsmentioning

confidence: 99%

Piperine Nanoparticles for Topical Application: Preparation, Characterization,In vitroandIn silicoEvaluation

Budama‐Kilinc

2019

ChemistrySelect

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“…In view of the previous rationale and in continuation of an ongoing program aiming at finding new structure leads with potential anti-inflammatory activities and selective COX-2 inhibition [22], new series of cyclic imides (1e13) have been synthesized and evaluated their in vitro COX-1/COX-2 inhibition, and in vivo assessment as anti-inflammatory activities (Fig. 1).…”

Section: Introductionmentioning

confidence: 99%

Synthesis, anti-inflammatory activity and COX-1/COX-2 inhibition of novel substituted cyclic imides. Part 1: Molecular docking study

Abdel‐Aziz

Eltahir

Asiri

2011

European Journal of Medicinal Chemistry

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“…Oximes are an important class of versatile ligands in coordination chemistry as they bear both nitrogen and oxygen donors that exhibit both hard and soft base characters. Oximes possess various biological and pharmaceutical activities, such as anti‐inflammatory, antioxidant, antitumor, bactericide, and fungicide properties.…”

Section: Introductionmentioning

confidence: 99%

Synthesis, spectroscopic, biological, and theoretical studies of new complexes from (E)‐3‐(2‐(5, 6‐ diphenyl‐1,2,4‐ triazin‐3‐ yl)hydrazono)butan‐2‐ one oxime

Samy

2020

Applied Organom Chemis

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New mononuclear Fe (III), Cu (II), Ag (I), ZrO ( IV) and UO2(VI) complexes were synthesized by the reaction of metal ions with (E)‐3‐(2‐(5, 6‐ diphenyl‐1,2,4‐ triazin‐3‐ yl)hydrazono)butan‐2‐ one oxime. The structures of the metal complexes were characterized using analytical, spectral (infrared, electronic, 1H NMR, electron spin resonance (ESR), and mass), magnetic moment, molar conductance, thermal gravimetric analysis, and powder X‐ray diffraction (XRD) measurements. All complexes have octahedral geometries except the Cu (II) complex, which has square planar geometry, and the UO2(VI) complex, in which the coordination number is seven. The ligand acts as a (neutral, monoanionic or dianionic) tridentate with N2O coordinating sites: N‐azomethine, N‐triazine, and O‐oxime. Fluorescence spectral studies were carried out in solid state and in dimethylformamide (DMF). The kinetic parameters of the thermal decomposition stages were calculated using Coats–Redfern equations. The morphological structures of the ligand and some complexes were determined using XRD. The molecular orbital calculations were carried out for the ligand and metal complexes using the Hyperchem 7.52 program on the basis of the PM3 level. The antimicrobial activities of the ligand and its complexes were investigated towards the microorganisms S. aureus and B. subtilis as Gram‐positive bacteria, S. typhimurium and E. coli as Gram‐negative bacteria, C. albicans, and A. fumigatus. The ligand and its complexes showed antitumor activity against Hep G‐2 cell lines, where Cu (II) and Ag (I) complexes seem to be promising as they showed IC50 values that are lower than and comparable to that of the antitumor drug doxorubicin.

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Synthesis and anti-inflammatory activity of novel (substituted)benzylidene acetone oxime ether derivatives: Molecular modeling study

Cited by 53 publications

References 17 publications

Piperine Nanoparticles for Topical Application: Preparation, Characterization,In vitroandIn silicoEvaluation

Piperine Nanoparticles for Topical Application: Preparation, Characterization,In vitroandIn silicoEvaluation

Synthesis, anti-inflammatory activity and COX-1/COX-2 inhibition of novel substituted cyclic imides. Part 1: Molecular docking study

Synthesis, spectroscopic, biological, and theoretical studies of new complexes from (E)‐3‐(2‐(5, 6‐ diphenyl‐1,2,4‐ triazin‐3‐ yl)hydrazono)butan‐2‐ one oxime

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