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Synthesis and biological activity evaluation of new isatin-gallate hybrids as antioxidant and anticancer agents (in vitro) and in silico study as anticancer agents and coronavirus inhibitors
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Background: The hybrid compounds hold promise for developing novel pharmaceuticals, potentially exhibiting greater activity, mainly against viruses and cancer diseases, than their components.

Objective: In this study, researchers explored the potential synergistic effects of hybrid molecules by designing and synthesizing a series of isatin-gallate hybrids, denoted as N’-(5-substituted-2-oxoindolin-3-ylidene)-3,4,5-trihydroxybenzohydrazide (3a–d).

Methods: Isatin-gallate hybrids (3a–d) were synthesized by reacting gallic hydrazide with each of the isatin analogs (2a–d). The structures of all produced compounds were described using spectrum methods such as fourier transform infrared (FTIR), 1H-nuclear magnetic resonance spectroscopy (1H-NMR), and physicochemical attributes. The evaluation of the tested hybrids (3a–d) involved assessing their in vitro antioxidant activities using the α, α-diphenyl-β-picrylhydrazyl (DPPH) free radical scavenging method and cytotoxic activities through the MTT [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] colorimetric assay for measuring cellular growth. Furthermore, in silico analysis was applied to the final hybrids to evaluate their effects as anticancer and anti-coronavirus agents.

Conclusion: Among the examined hybrid compounds, 3b demonstrated substantial in vitro antioxidant and cytotoxic activities. In silico analysis revealed slight variations in the anticancer activity of compounds 3a–d, with differing affinities observed across various cancer cell lines. Additionally, these compounds exhibited moderate efficacy in inhibiting coronavirus activity.

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Publication Date
Thu Aug 17 2023
Journal Name
Journal Of Thermoplastic Composite Materials
Fabrication and characterization of PEKK nanocomposites: An in vitro study
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Although the number of implants has increased gradually and consistently over the years to around one million per year globally, there is still far more potential for advancement in the field of dental implantology which is typically growing quickly. This study investigates the effect of nanofiller reinforcement high-performance polymer matrix to enhance mechanical and physical characteristics. Calcium silicate (CS)/Polyetherketoneketone (PEKK) biomedical composite (G0 as a control group) is reinforced with different weight percentages (G1-G4) of tellurium dioxide nanoparticles (TeO2NPs) ( n = 5). This research uses ethanol as a binder for mixing various weight percentages (wt%) of TeO2NPs w

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Publication Date
Wed May 29 2024
Journal Name
Pharmacia
Formulation, in vitro and in vivo evaluation of olanzapine nanoparticles dissolving microneedles for transdermal delivery
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Olanzapine (OLZ) is classified as a typical antipsychotic drug utilized for the treatment of schizophrenia. Its oral bioavailability is 60% due to its low solubility and pre-systemic metabolism. Hence, the present work aims to formulate and evaluate OLZ nanoparticles dissolving microneedles (MNs) for transdermal delivery to overcome the problems associated with drug administration orally. OLZ nanoparticles were prepared by the nanoprecipitation method. The optimized OLZ nanoparticle formula was utilized for the fabrication of dissolving MNs by loading OLZ nanodispersion into polydimethylsiloxane (PDMS) micromould cavities, followed by casting the polymeric solution of polyvinylpyrrolidone(PVP-K30) and polyvinyl alcohol (PVA) to form

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Publication Date
Sun Jun 05 2016
Journal Name
Baghdad Science Journal
Synthesis, Characterization and Study of Antibacterial Activity of a New Schiff Base Ligand and Its Complexes with Co(II), Ni(II), Cu(II), Cd(II) and Hg(II) Metal Ions
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Some coordination complexes of Co(??), Ni(??), Cu(??), Cd(??) and Hg(??) are reacted in ethanol with Schiff base ligand derived from of 2,4,6- trihydroxybenzophenone and 3-aminophenol using microwave irradiation and then reacted with metal salts in ethanol as a solvent in 1:2 ratio (metal: ligand). The ligand [H4L] is characterized by FTIR, UV-Vis, C.H.N, 1H-NMR,13C-NMR, and mass spectra. The metal complexes are characterized by atomic absorption, infrared spectra, electronic spectra, molar conductance, (C.H.N for Ni(??) complex) and magnetic moment measurements. These measurements indicate that the ligand coordinates with metal (??) ion in a tridentate manner through the nitrogen and oxygen atoms of the ligand, octahedral st

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Publication Date
Sun Jun 05 2016
Journal Name
Baghdad Science Journal
Synthesis, Characterization and Study of Antibacterial Activity of a New Schiff Base Ligand and Its Complexes with Co(II), Ni(II), Cu(II), Cd(II) and Hg(II) Metal Ions
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Some coordination complexes of Co(??), Ni(??), Cu(??), Cd(??) and Hg(??) are reacted in ethanol with Schiff base ligand derived from of 2,4,6- trihydroxybenzophenone and 3-aminophenol using microwave irradiation and then reacted with metal salts in ethanol as a solvent in 1:2 ratio (metal: ligand). The ligand [H4L] is characterized by FTIR, UV-Vis, C.H.N, 1H-NMR,13C-NMR, and mass spectra. The metal complexes are characterized by atomic absorption, infrared spectra, electronic spectra, molar conductance, (C.H.N for Ni(??) complex) and magnetic moment measurements. These measurements indicate that the ligand coordinates with metal (??) ion in a tridentate manner through the nitrogen and oxygen atoms of the ligand, octahedral structures

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Publication Date
Sun Jun 05 2016
Journal Name
Baghdad Science Journal
Synthesis, Characterization and Study of Antibacterial Activity of a New Schiff Base Ligand and Its Complexes with Co(II), Ni(II), Cu(II), Cd(II) and Hg(II) Metal Ions
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Some coordination complexes of Co(ІІ), Ni(ІІ), Cu(ІІ), Cd(ІІ) and Hg(ІІ) are reacted in ethanol with Schiff base ligand derived from of 2,4,6- trihydroxybenzophenone and 3-aminophenol using microwave irradiation and then reacted with metal salts in ethanol as a solvent in 1:2 ratio (metal: ligand). The ligand [H4L] is characterized by FTIR, UV-Vis, C.H.N, 1H-NMR,13C-NMR, and mass spectra. The metal complexes are characterized by atomic absorption, infrared spectra, electronic spectra, molar conductance, (C.H.N for Ni(ІІ) complex) and magnetic moment measurements. These measurements indicate that the ligand coordinates with metal (ІІ) ion in a tridentate manner through the nitrogen and oxygen atoms of the ligand, octahed

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Publication Date
Mon Mar 20 2023
Journal Name
Liquid Crystals
Synthesis and study the mesomorphic behaviour of some new 1,3,4-thiadiazoline derivatives
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Investigation of mesomorphic properties of new 1,3,4-thiadiazolines (which are synthesised via many steps in Scheme 1) was carried out in this study. These compounds are designed to have a heterocyclic unit, a carboxylate linkage group and a polar ether chain at the end of the molecule adjacent to the benzene ring, which enhance the dipolar interactions forces (varied from one to eight carbons) to investigate the association properties of their phases. The structure of the target compounds and the intermediates were confirmed by 1H NMR, 13C NMR, mass and FTIR spectral techniques. Polarised microscopic studies revealed that all the compounds in the series exhibited enantiotropic liquid crystalline properties. This was further confirmed using

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Publication Date
Sat Jun 01 2024
Journal Name
Minar International Journal Of Applied Sciences And Technology
PREPARATION, CHARACTERIZATION AND EVALUATE THEIR BIOLOGICAL ACTIVITY OF NEW HETEROCYCLIC COMPOUNDS DERIVED FROM 4-((1-(4-HYDROXYPHENYL) ETHYLIDENE) AMINO) BENZENESULFONAMIDE
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The research included the preparation of cyclic compounds from thiazoles, imidazoles and oxazepines from the reaction of cyclization starting material that acts Schiff bases, which is a raw material in the formation of cyclic compounds from Schiff's(B1) by reaction of 4- aminobenzenesulfonylamide with 4-hydroxyacetophenone which can used to synthesized two lines. The first introducing the preparation of pyrazoles [B4, B5] from ester [B2], which derived to acid hydrazide[B3] with hydrazine hydrate and final pyrazoles obtained by the reaction with diethylmalonate and acetylacetone. The second including prepared the new 1,3-oxazepine1,5-dione derivatives[B6,B7,B8] from adding different anhydrides to the base[B1] as a seven membered ring ; te

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Publication Date
Sun Mar 02 2008
Journal Name
Baghdad Science Journal
In vitro antimicrobial activity of total sesquiterpene lactones and phenols isolated from some Iraqi plants
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The antimicrobial potency of the crude ethanolic extracts from different Iraqi plants were evaluated . Further more, total sesquiterpene lactones and phenolic compounds were isolated and their antimicrobial activity attempted. The results indicated that crude extracts have no activity except that of Callistemon lanceolatus. Also, the sesquiterpene lactones and phenolic compounds isolated from Callistemon lanceolatus were the most significant antimicrobial active constituents of the studied plants.

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Publication Date
Mon Sep 02 2024
Journal Name
F1000research
Green synthesis of gold nanoparticles using Pelargonium Graveolens leaf extract: characterization and anti-microbial properties (An in-vitro study)
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Background In recent years, there has been a notable increase in the level of attention devoted to exploring capabilities of nanoparticles, specifically gold nanoparticles AuNPs, within context of modern times. AuNPs possess distinct biophysical properties, as a novel avenue as an antibacterial agent targeting Streptococcus Mutans and Candida Albicans. The aim of this study to create a nano-platform that has the potential to be environmentally sustainable, in addition to exhibiting exceptional antimicrobial properties against Streptococcus Mutans as well as Candida Albicans. Methods this study involved utilization of Pelargonium Graveolens leaves extract as a cost effective and environmentally sustainable app

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Publication Date
Tue Feb 28 2023
Journal Name
Research Journal Of Pharmacy And Technology
Synthesis and Characterization of Molecularly Imprinted Polymers for Metronidazole by using Allyl Chloride and Allyl Bromide as Monomers
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Metronidazole-MIPs were prepared by using (MDZ) as the template as well as allylchloride (AYC) or allylbromide (AYB) as monomer, used (TMPTA) tri-methylol propane tri-acrylate or ethylene glycol di-methyl acrylate (EGDMA) as cross-linker and initiator used (BP) benzyl peroxide. By using different plasticizers (di butyl Phthalate (DBPH), Nitrobenzene (NB), oleic acid (OA) and paraffin) for MDZ-MIP1 and (Di-butyl sebecate (DBS), Di-methyl acrylate (DMA), Tributylphosphate(TBP) and Tris(ethylhexyl phosphate (TEHP) ) for MDZ-MIP2. Membranes of MIPs were prepared in PVC matrix. The characterizations of each electrode were determined The Slope range from (55.083 - 43.711) mV/decade, Limit of Detection (8 X 10 -4- 2 X 10-6) and Linearity

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