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).
الصيغة العامة للمعقدات الجديدة [M2(BDS)Cl4] الناتجة من تفاعل الليكاند الجديد] ن1,ن4-ثنائي(1أ –بنزو]د[ اميدازول-2-يل)-ن1,ن4-ثنائي(4-ثنائي مثيل امينو) بنزيل) سكسنمايد[ (BDS) مع الايونات الفلزية الكادميوم, الكوبلت, الزئبق, النحاس والنيكل. تم اشتقاق هذا الليكاند من تفاعل المواد الثلاث 4-(ثنائي ميثيل أمينو) بنزالدهيد، 2-أمينو بنزيميدازول، وكلوريد السكسينيل. تم تشخيص المركبات باستخدام مطيافية طيف الاشعة تحت الحمراء وطيف الرن
... Show MorePolyimides are widely used in high-temperature plastics, adhesives, dielectrics, photoresists, nonlinear optical materials, separation membrane materials, and Langmuir-Blodgett (LB) films. They are commonly regarded as the most heat-resistant polymers. This work involved the synthesis of a new bismaleimide homopolymer and copolymer by performing many steps. The synthesis of compound (1) (bis [4-(amino phenyl) Schiff base] tolidine) via condensation of o-tolidine with two moles of 4-aminoacetophenone. Secondly, compound (1) was combined with maleic anhydride to form compound (2) (4, 4ˉ-bis[4-(N-maleamic acid) phenyl Schiff base] toluidine). Thirdly, a dehydration reaction was carried out affording compound (3) (4,4ˉ-bis [4-(N-maleimidyl
... Show MoreThis article includes designed and synthesized for bent-shaped liquid crystal molecules starting from 5,5-diethylpyrimidine-2,4,6(1H,3H,5H)-trione and two moles of chloroacetylchloride in N, N-dimethyl formamide (DMF) and triethylamine (TEA) to product compound [I] ,then reacted the later compound with two moles of 4-hydroxybenzonitrile to yield nitrile compound [II]. Likewise, reaction 5,5-diethylpyrimidine-2,4,6(1H,3H,5H)-trione and two moles of ethylchloroacetate with fused sodium acetate in ethanol to create an ester compound [III], and then the later compound was reacted with two moles of hydrazine hydrate in ethanol to obtained hydrazide acid compound [IV]. After that, the compound [IV] reacted with two moles of ethyl acetoacetate in
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The present investigation aimed to formulate a liquid self-microemulsifying drug delivery system (SMEDDS) of tacrolimus to enhance its oral bioavailability by improving its dispersibility and dissolution rate. Four liquid SMEDDS were prepared using maisine CC as oil phase, labrasol ALF as surfactant and transcutol HP as co-surfactant based on the solubility studies of tacrolimus in these components. The phase behavior of the components and the area of microemulsion were evaluated using pseudoternary phase diagrams. The formulations were also assessed for thermodynamic stability, robustness to dilution, self-emulsification time, drug content, globule size and polydispersity index. The prepared SMEDDS formulations exhibi
... Show MoreIn-vitro biological activities of the free new H4L ( indole-7-thiocarbohydrazone) ligand and its Ni(II), Pd(II) , Pt(II), Cu(II), Ag(I), Zn(II) and Cd(II) complexes are screened against two cancerous cell lines, that revealed significant activity only for [Cu2Cl2(H4L)2(PPh3)2] after 72 h treatment by the highest tested concentrations. The Copper(I) complex was characterized by X-ray Crystallography and the NMR spectra, whereas it has been confirmed to have momentous cytotoxicity against ovarian, breast cancerous cell lines (Caov-3, MCF-7). The apoptosis-inducing properties of the Cu(I) complex have been investigated through fluorescence microscopy visualization, DNA fragmentation analysis and propidium iodide flow cytometry.
ABSTRACT : A new ligand [ 2- (3-acetylthioureido)-3-phenylpropanoic acid (APA) is synthesized by reaction of acetyl isothiocyanate with phenylalanine (1:1). It is characterized by micro elemental analysis (C.H.N.S.), FT-IR, (UV-Vis) and 1H and 13CNMR spectra. Some metals ions complexes of this ligand were prepared and characterized by FT-IR, UV-Visible spectra, conductivity measurements, magnetic susceptibility and atomic absorption. From results obtained, the following formula [M(APA)2] where M2+ = Mn, Co, Ni, Cu, Zn, Cd and Hg, the proposed molecular structure for these complexes as tetrahedral geometry, except copper complex is has square planer geometry.
New schiff bases series (VIII) a-e and 1,3-thiazolidin-4-one derivatives (IX) a-e containing the 1,2,4-triazole and 1,3,4-thiazazole rings were synthesized and screening their biological activities. These compounds were identified via Fourier transform infrared (FT-IR) spectra, some via Proton nuclear magnetic resonance (1H-NMR) and mass spectra. The biological results indicated that all of these compounds did not reveal antibacterial effectiveness against (Escherichia coli and Klebsiella species) (G-). Some of these compounds showed moderate antibacterial activity against (Staphylococcus aureus, and Staphylococcus epidermidis) (G+), and all compounds exhibited moderate activity against Candida albicans.
Acid dissociation constants of some Schiff bases derived from 4, 6-dimethyl 2-amino pyrimidine of the type (1) in 50% V/V dioxane-water mixture in 0.003M KCl, at three different temperatures were determined potentiometrically. The thermodynamic energies were calculated and a good linear correlation was obtained between pKa and IR OH. Stretching frequencies.
New bidentate Schiff base ligand (L) namely [(Z)-3-(2-oxoindolin-3ylildeneamino)benzoic acid] type (NO) was prepared via condensation of isatin and 3-amino benzoic acid in ethanol as a solvent in existence of drops of (glac. CH3COOH). The new ligand (L) was characterized base on elemental microanalysis, FT-IR, UV-Vis, 1H-NMR spectra along with melting point. Ligand complexes in general formula [M(L)2Cl2]. H2O, where: MII = Co, Cu, Cd, and Hg; L= C15H10 N2O3 were synthesized and identified by FT-IR, UV-Vis, 1H-NMR (for Cd complex only) spectra, atomic absorption, chloride content along with molar conductivity and magnetic susceptibility. It was found that the ligand behaves as bidentate on complexation via (N) atom of imine group an
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