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).
Mefenamic acid (MA) is one of the non-steroidal anti-inflammatory drugs, it is widely used probably due to having both anti-inflammatory and analgesic activity, the main side effects of mefenamic acid include gastrointestinal tract (GIT) disturbance mainly diarrhea, peptic ulceration, and gastric bleeding. The analgesic effects of NSAIDs are probably linked to COX-2 inhibition, while COX-1 inhibition is the major cause of this classic adverse effects. Introduction of thiazolidinone may lead to the increase in the bulkiness leads to the preferential inhibition of COX-2 rather than COX-1 enzyme. The study aimed to synthesize derivatives of mefenamic acid with more potency and to decrease the drug's potential side effects, new series of 4-t
... Show More4,4'-(pyridine-2,6-diylbis(1,3,4-oxadiazole-5,2-diyl))bisphenol monomer (3)was synthesized from cyclization of N'2,N'6-bis(4-hydroxybenzylidene)pyridine-2,6-dicarbohydrazide (2)in the presence of bromine in glacialacetic acid. Newly five polymers (P1-P5) were synthesized from reaction bis-1,3,4-oxadiazole bisphenolmonomer with five different di acid chloride. The antibacterial activity of the synthesized polymers was screened against gram positive and gram negative bacteria. Polymers P4 and P5 exhibited significant antibacterial against all microorganisms, as well these polymers showed highest antifungal activity.
New nitrone and selenonitrone compounds were synthesized. The condensation method between N-(2-hydroxyethyl) hydroxylamine and substituted carbonyl compounds such as [benzil, 4, 4́-dichlorobenzil and 2,2́ -dinitrobenzil] afforded a variety of new nitrone compounds while the condensation between N-benzylhydroxylamine and substituted selenocarbonyl compounds such as [di(4-fluorobenzoyl) diselenide and (4-chlorobenzoyl selenonitrile] obtained selenonitrone compounds. The condensation of N-4-chlorophenylhydroxylamine with dibenzoyl diselenide obtained another type of selenonitrone compounds. The structures of the synthesized compounds were assigned based on spectroscopic data (FT-IR,
... Show MoreIn this research, a new 1, 3, 4-Thiadiazole derivatives have been synthesized by many heterocyclic reactions. Starting from (2, 5 – dimercapto -1, 3, 4-Thiadiazole) a variety of derivatives have been synthesis. Compound (1) was synthesized by the reaction of hydrazine hydrate with carbon disulphide in absolute ethanol. The compound (1) was reacted with 1, 2-dibromoethane in presence of alkali ethanol to give the compound (2). The compound (3) was formed from the reaction of compound (2) with hydrazine hydrate. Schiff base (4) was obtained by reacting of compound (3) with the compound (p-hydroxybenzaldehyde) in absolute ethanol. A variety of phenolic Schiff base (Methylolic, Etheric, and Epoxy) derivatives have been synthesized. Methylol
... Show MoreThe synthesized ligand [4-chloro-5-(N-(5,5-dimethyl-3-oxocyclohex-1-en-1-yl)sulfamoyl)-2-((furan-2-ylmethyl)amino)benzoic acid] (H2L1) was identified utilizing Fourier transform infrared spectroscopy (FT-IR), 1 H, 13 C – NMR, (C.H.N), Mass spectra, UVVis methods based on spectroscopy. To detect mixed ligand complexes, analytical and spectroscopic approaches such as micro-analysis, conductance, UV-Visible, magnetic susceptibility, and FT-IR spectra were utilized. Its mixed ligand complexes [M(L1)(Q)Cl2] [ where M= Co(II), Ni(II) , and Cd(II)] and complexes [Pd(L1)(Q)] and [Pt(L1)(Q)Cl2]; [H2L1] =β-enaminone ligand =L1 and Q= 8-Hydroxyquinoline = L2]. The results showed that the complexes were synthesised utilizing the molar ratio M: L1
... Show MoreThe reaction oisolated and characterized by elemental analysis (C,H,N) , 1H-NMR, mass spectra and Fourier transform (Ft-IR). The reaction of the (L-AZD) with: [VO(II), Cr(III), Mn(II), Co(II), Ni(II), Cu(II), Zn(II), Cd(II) and Hg(II)], has been investigated and was isolated as tri nuclear cluster and characterized by: Ft-IR, U. v- Visible, electrical conductivity, magnetic susceptibilities at 25 Co, atomic absorption and molar ratio. Spectroscopic evidence showed that the binding of metal ions were through azide and carbonyl moieties resulting in a six- coordinating metal ions in [Cr (III), Mn (II), Co (II) and Ni (II)]. The Vo (II), Cu (II), Zn (II), Cd (II) and Hg (II) were coordinated through azide group only forming square pyramidal
... Show MoreA new methodology was applied to the synthesis of new imidazolones and oxyazepine derivatives containing imidazo thiazole fused rings. Starting with 5-(4-bromo phenyl) imidazo (2, 1-b) thiazole, which was synthesized using the standard procedure, the Carbaldehyed group was introduced at position 6 of 5-(4-bromo phenyl) imidazo (2, 1-b) thiazole. Then, this 6-carbaldehyed derivative was condensed with different substituted aromatic amines to afford new Schiff bases. The latter were cyclized into new oxazepine and imidazolone derivatives by using phthalic anhydride and glycine, respectively. These new derivatives were characterized by using FT-IR, 1HHNMR, and 13CNMR spectra, as well as examined (evaluated) for anti-bacterial and anti-fungal a
... Show MoreIn this work, some of new 2-benzylidenehydrazinecarbothioamide derivatives have been prepared by condensation of thiosemicarbazide and different substituted aromatic benzaldehydes in presence of glacial acetic acid to give compounds (1-6), these compounds have characterized by its physical properties and spectroscopic methods. This work also included theoretical study to prove the ability of these compounds as corrosion inhibitors; The program package of Gaussian 09W with its graphical user interface GaussView 5.0 had used for this purpose; the methods of Density Functional Theory (DFT) with basis set of 6-311G (d,p) / hybrid function of B3LYP and semiempirical method of PM3 have been used, the study included theoretical simulation
... 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.