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).
Background: Frovatriptan succinate (FVT) is an effective medication used to treat migraines; however, available oral formulations suffer from low permeability; accordingly, several formulations of FVT were prepared. Objective: Prepare, optimize, and evaluate FVT-BE formulation to develop enhanced intranasal binary nano-ethosome gel. Methods: Binary ethosomes were prepared using different concentrations of phospholipid PLH90, ethanol, propylene glycol, and cholesterol by thin film hydration and characterized by particle size, zeta potential, and entrapment efficiency. Furthermore, in-vitro, in-vivo, ex-vivo, pharmacokinetics, and histopathological studies were done. Results: Regarding FVT-loaded BE, formula (F9) demonstrated the best paramet
... Show MoreThe compound [G1] was prepared from the reaction of thiosemicarbazide with para-hydroxyphenylmethyl ketone in ethanol as a solvent. Then by sequence reactions prepared [G2] and [G3] compounds. The compound [G4] reaction with ethyl acetoacetoneto synthesized compound [G6] and acetyl acetone to synthesized compound [G5]. Reaction the [G3] with two different types of aldehydes in the present of pipredine to form new alkenes compounds [G7]and [G8].The compound [G3] reacted with hydrazine hydrate to formation[G4] with present the hydrazine hydrade 80% in (10) ml of absolute ethanol. Latter the compound [G4]reacted with different aldehydes with present the glacial acetic acid and the solvent was ethanol to formed the Schiff bases compounds[G9] an
... Show MoreThe compound [G1] was prepared from the reaction of thiosemicarbazide with para-hydroxyphenylmethyl ketone in ethanol as a solvent. Then by sequence reactions prepared [G2] and [G3] compounds. The compound [G4] reaction with ethyl acetoacetoneto synthesized compound [G6] and acetyl acetone to synthesized compound [G5]. Reaction the [G3] with two different types of aldehydes in the present of pipredine to form new alkenes compounds [G7]and [G8].The compound [G3] reacted with hydrazine hydrate to formation[G4] with present the hydrazine hydrade 80% in (10) ml of absolute ethanol. Latter the compound [G4]reacted with different aldehydes with present the glacial acetic acid and the solvent was ethanol to formed the Schiff bases compounds[G9] an
... Show MoreThe amino thiadiazole [I] on treatment with aromatic aldehydes yielded Schiff bases [IIa-c], which cyclized to thiazolidinone [IIIa-c] derivatives by reaction with thioglycolic acid. Reaction of carbon disulfide and methyl iodide with [I] gavedithiomethyl [IV] which on treatment with o-phenylenediamine gave the condensed N-Imidazolythiadiazolylamine [V], However, reaction of [I] with phenylisocyanate and phenylisothiocyanate afforded the carbamideand carbothiamide derivatives [VI. VII] ac. The structure of these compounds was characterized from their melting point, FTIR spectroscopy and elementalanalysis
New N2O2 donor kind Schiff basehas been destined and structured by reaction Ampyrone with O-hydroxyacetophenone and Anthranilic acid. The metal complexes of the Schiff base with Mn(II), Hg(II), Ni(II), Cu(II), and Co(II) metal ions were designed and characterized by magnetic susceptibility, elemental analyses, molar conduction, IR, and 1H NMR,UV-Vis spectral metrics.The UV-Vis. and magnetic susceptibility data of the complexes suggest a square-planar, tetrahedraland octahedral geometries around the central metal ions. All elaborations were accomplished after determination the optimum molar concentration and pH which followed law of Lambert-Beer's in the researches pH scopes. The composition of these complexes were conclude dapprobating to t
... Show MorePolymer metal complexes of poly ethylene glycol acetal and Ag (I), Cu (II), Ni (II), Mn (II), Co (III) and Hg (II) were prepared from the reaction of PEG with aldehyde derived fromErythro-ascorbic acid (pentulosono-ɣ-lactone-2, 3- enedianisoate). All these compounds were characterized by Thin Layer Chromatography (TLC) and FTIR spectra and aldehyde was also characterized by (U.V-Vis), 1HNMR,13CNMR, and mass spectra. It has been established that, the polymer and its metal complexes showedgood activities against four pathogenic bacteria (Escherichia coli , Klebsiellapneumonae,Staphylococcusaureus, Staphylococcus Albus) and two fungal (Aspergillus Niger,Yeast). The polymer metal complexes showed higher activity than the free polymer.Theorder
... Show MorePolymer metal complexes of poly ethylene glycol acetal and Ag (I), Cu (II), Ni (II), Mn (II), Co (III) and Hg (II) were prepared from the reaction of PEG with aldehyde derived from Erythro-ascorbic acid (pentulosono-ɣ-lactone-2, 3- enedianisoate). All these compounds were characterized by Thin Layer Chromatography (TLC) and FTIR spectra and aldehyde was also characterized by (U.V-Vis), 1HNMR,13CNMR, and mass spectra. It has been established that, the polymer and its metal complexes showed good activities against four pathogenic bacteria (Escherichia coli ,Klebsiellapneumonae, Staphylococcusaureus, Staphylococcus Albus) and two fungal (Aspergillus Niger,Yeast). The polymer metal complexes showed higher activity than the free polymer. The
... Show More2,2'-(1-(3,4-bis(carboxydichloromethoxy)-5-oxo-2,5-dihydrofuran-2-yl)ethane-1,2-diyl)bis(oxy)bis(2,2-dichloroacetic acid) a derivative of L-ascorbic acid was prepared by reaction of L-ascorbic acid with trichloroacetic acid (1:4) ratio, in the presence of potassium hydroxide. A series of new metal complexes of this ligand were prepared by a reaction with the chlorides of Cd(II), Co(II), Ni(II), Cu(II) and Zn(II). The new ligand and its complexes were identified by C.H.N., IR, UV-visible spectra, Thermogravimetric analysis (TGA), as well as 1H, 13C-NMR and Mass spectra for ligand L. The complexes were also identified by molar conductance, atomic absorption, magnetic susceptibility and X-ray diffraction for Cu (II) complex. FT-IR spectra
... Show MoreAlginate is one of the natural biopolymers that is widely used for drug formulations, combination of alginate with other polymers, such as gum acacia, pectin, and carrageenan can increase mechanical strength, therefore, can reduce leakage of the encapsulated active pharmaceutical ingredient from the polymer matrix. Interaction of alginate and these polymers can occur via intermolecular hydrogen bonds causing synergism, which is determined from the viscosity of polymer mixture.
Alginate was combined with gum acacia/pectin/carrageenan in different blending ratios (100:0, 75:25, 50:50, 25:75, and 0:100) with and without addition of CaCl2. The synergism effect is obtained from the design of experimental (DoE), and calculati
... Show MoreObjective: The goal of this research is to load Doxorubicin (DOX) on silver nanoparticles coupled with folic acid and test their anticancer properties against breast cancer. Methods: Chitosan-Capped silver nanoparticles (CS-AgNPs) were manufactured and loaded with folic acid as well as an anticancer drug, Doxorubicin, to form CS-AgNPs-DOX-FA conjugate. AFM, FTIR, and SEM techniques were used to characterize the samples. The produced multifunctional nano-formulation served as an intrinsic drug delivery system, allowing for effective loading and targeting of chemotherapeutics on the Breast cancer (AMJ 13) cell line. Flowcytometry was used to assess therapy efficacy by measuring apoptotic induction. Results: DOX and CS-Ag
... Show More