Objective: This study involved the synthesis of new Schiff bases and 1,3-oxazepine derivatives from the baclofen drug and study the anticancer activities. Methods: Baclofen was initially reacted with aromatic aldehydes to create Schiff base derivatives (Ia–Ib), which were then closed in the next step using anhydrous acids to form oxazepine derivatives (IIa–IId). Results: The title compounds were synthesized successfully and identified using FT-IR, 1H NMR, and 13C NMR spectroscopy. Additionally, compound (IIc)’s (3-(4-chloro-phenyl)-4-[2-(4nitro-phenyl)-4,7-dioxo-4,7-dihydro-[1,3] oxazepin-3-yl]butyric acid) anticancer activity was assessed using MTT assay against FTC-133 (thyroid cancer) compared with WRL-68 (normal cell line). Discussion: The results showed that the viability of the FTC-133 cell was found to be greatest at 12.5 g/mL (96.52 ± 0.70) and lowest at 400 g/mL (35.378 ± 5.07). The effect of compound (IIc) on the normalizing of the WRL-68 cell line resulted in an IC50 for 62.39 ϻg/mL. Conclusions: It has been found that the compound (IIc) has good efficiency against thyroid cancer (FTC-133).
The Co(II), Ni(II) ,Cu(II), Zn(II) ,Cd(II) and Hg(II) complexes of mixed of amino acid (L-Proline ) and Trimethoprim antibiotic were synthesized. The complexes were characterized using solubility, melting point, conductivity measurement ,. and determination the percentage of the metal in the complexes by flame(AAS).Magnetic susceptibility, Spectroscopic Method [FT-IR and UV-Vis]. Draw the proposed structure of the complexes using program , Chem. office 3D(2006). The ligands and there metal complexes were screened for their antimicrobial activity against four bacteria (gram + ve) and (gram -ve){Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus and Bacillus}.The proposed structure of the complexes using program , Chem office 3D(
... Show MoreThe Co(II), Ni(II) ,Cu(II), Zn(II) ,Cd(II) and Hg(II) complexes of mixed of amino acid (L-Proline) and Trimethoprim antibiotic were synthesized. The complexes were characterized using solubility, melting point, conductivity measurement ,. and determination the percentage of the metal in the complexes by flame(AAS).Magnetic susceptibility, Spectroscopic Method [FT-IR and UV-Vis]. Draw the proposed structure of the complexes using program , Chem. office 3D(2006). The ligands and there metal complexes were screened for their antimicrobial activity against four bacteria (gram + ve) and (gram-ve){Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus and Bacillus}.The proposed structure of the complexes using program , Chem office 3D(20
... Show MorePulsatile drug delivery systems are time-controlled dosage forms which are designed to release the active pharmaceutical ingredient after a predetermined lag time to synchronize the disease circadian rhythm. A migraine shows circadian rhythm with a marked increase in attacks between 6 a.m. and 8 a.m.
Sumatriptan is a selective agonist at serotonin (5-Hydroxy tryptamine1 (5-HT1))receptors, is an effective treatment for acute migraine attacks.
The aim of this work is to prepare time-controlled press-coated tablet with a lag time of 5.45 hrs.
Six formulas of fast dissolving core tablets and three formulas of press-coated tablets were prepared by using direct compression method using different variables to prepa
... Show MorePolycyclicacetal was prepared by the reaction of PEG with 4-nitrobenzaldehyde. Cobalt was used for producing a polymer metal complex and solution casting was used to produce a polymer blend including nano chitosan. All produced compounds have been characterized by FT-IR, DSC/ TGA, and SEM techniques as well as biological activity. The production of polyacetal is illustrated by the FT-IR analysis. The DSC/TGA results indicate the prepared polymer blends' thermal stability. Staphylococcus aureas, Klebsiella pneumoniae, Bacillus subtilis, and Escherichia coli were the four types of bacteria selected to study and evaluate the antibacterial activity of produced polyacetal, its metal complex, and polymer blend. Results indicates that ther
... Show MoreAbstract. In this work, Bi2O3 was deposited as a thin film of different thickness (400, 500, and 600 ±20 nm) by using thermal oxidation at 573 K with ambient oxygen of evaporated bismuth (Bi) thin films in a vacuum on glass substrate and on Si wafer to produce n-Bi2O3/p-Si heterojunction. The effect of thickness on the structural, electrical, surface and optical properties of Bi2O3 thin films was studied. XRD analysis reveals that all the as deposited Bi2O3 films show polycrystalline tetragonal structure, with preferential orientation in the (201) direction, without any change in structure due to increase of film thickness. AFM and SEM images are used to investigate the influences of film thickness on surface properties. The optical measur
... Show MoreIn this research, cyclic compounds derived from 2- furfural mercaptan (oxazole, triazoles) were synthesized, and their biological efficacy was measured and compared with standard drugs. Also, their effectiveness as anti-oxidant was measured and compared with ascorbic acid as a standard substance. Some of the synthesized compounds were deduced with good efficacy. © 2021 Sami Publishing Company. All rights reserved
This work include synthesized and characterization the compound [I] by reaction 1,4-phenylenediamine with chloro acetic acid then this compound reaction with methanol in present sulfuric acid to synthesized ester compound [II] after that reaction with hydrazine hydrate to synthesized acide hydrazide [III] and the later compound reaction with substituted acetophenone[IV]n to synthesized substituted acetophenone hydrazones[V-XI]. In addition synthesized4-formylpyrazole derivatives [XIIXVIII] via cyclisation substituted acetophenone hydrazones [V-XI] with Vilsmeier-Haack reagent DMF/POCl3. The compounds characterized by melting points, FTIR, 1HNMR and mass spectroscopy. The mesomorphic behavior studied by using polarized optical microscopy and
... Show MoreTwo compounds,[2-amino-4-(4-nitro phenyl) 1,3-thiazole],(4) and [2-amino-4-(4-bromo phenyl) 1,3-thiazole],(5), were synthesized by refluxing thiourea (1) with each of para-ntiro and para-bomophanacyl bromides(2) and (3) respectively, in absolute methanol. Then, by reaction of [5] with 3,5-dinitrobenzoyl chloride in dimethylformamide (DMF) yielded (6) .On the other hand, reaction of (4) with chloroacetyl chloride in dry benzene afforded (7), which is upon treatment with thiourea in absolute methanol, af
... Show MoreA tetradentate (N2O2) Schiff base (H2Ldfm) was successfully synthesized via condensation of curcumin / diferuloylmethane (dfm) and L-leucine amino acid (HL). There were three different methods that used for synthesizing H2Ldfm; (refluxing, grading, and fusion). Ten different metal complexes were also successfully synthesized by combination of the Schiff base (H2Ldfm) and 1,10-phenanthroline (phen) ligand to form a hexadentate (N4O2) mixed ligands (Ldfm , phen) with ten different metal salts (M) where{ M= Al(III), Mn(II), Fe(III), Co(II), Ni(II), Cu(II), Ag(I), Cd(II), Hg(II), and Pb(II)}. The molar ratio of reactants was (1:1:1) (M: H2Ldfm : phen). The new Schiff base and its new complexes were characterized by different physicochemical tec
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