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 aim of this work is the synthesis of new Schiff base derived from PVA and Erythro-ascorbic acid derivative (pentulosono-ɣ-lactone-2,3-enedianisoate) and its metal complexes of biological significance. All synthesized 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. The synthesized Schiff base & its metal complexes were screened for their in vitro antimicrobial activity against five pathogenic bacteria (Escherichia coli, Shigella dysentery,Klebsiellapneumonae,Staphylococcusaureus, Staphylococcus Albus) and two fungal (Aspergillus Niger,Yeast).The biological activity ofall complexes is higher than free Schiff base ligand andf
... Show MorePiroxicam (PIR) is a nonsteroidal anti-inflammatory drug of oxicam category, used in gout, arthritis, as well as other inflammatory conditions (topically and orally). PIR is practically insoluble in water, therefore the aim is prepare and evaluate piroxicam as liquid self-nanoemulsifying drug delivery system to enhance its dispersibility and stability. The Dispersibilty and Stability study have been conducted in Oil, Surfactant and Co-surfactant for choosing the best materials to dissolve piroxicam. The pseudo ternary phase diagrams have been set at 1:1, 2:1, 3:1 as well as 4:1 ratio of surfactants and co-surfactants, also there are 4 formulations were prepared by using various concentrations of transcutol HP, cremophore EL and triacetin
... Show MoreThe outstanding evidence of phthalimide pharmacophore in securing enhanced biological activities had encouraged further research and development into phthalimide-based derivatives as potential new drugs. In this study, phthalimide core was hybridized with aldehydes giving integrated imines displaying different types of functionalities and at alternating positions. The resulting compounds, therefore, provide an innovative window to explore possible differential biological effects as antioxidants and anticancer agents. A total of sixteen compounds were synthesized, and each was verified by FT-IR, H NMR, C NMR, and MS characterization. Herein, a facile single-step synthesis method was employed substituting the conventional two-step che
... 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 MoreNew chlropheniramine maleate (CPM) selective electrochemical membranes were prepared by using chlropheniramine maleate -molecularly imprinted polymers. MIP was prepared by bulk polymerization using 2-hydroxyethyl methacrylate (2-HEMA) as monomer, ethylene glycol dimethacrylate (EGDMA) as a cross-linker and a benzoyl peroxide (BPO) as an initiator at 600C. Three CPM-MIP electrodes were constructed by using tri-tolyl Phosphate (ToCP), tris (2- ethyl hexyl) Phosphate (TEHP) and tributyl Phosphate (TBP) as plasticizers in PVC matrix.Electrode parameters including slopes, working concentrations ph. The interference effect in the presence of (Na+, Mg+2, Al+3, Glycine, Alanine, Arginine and Phenylalanine) was studied using the separated a
... Show Morecharacteristic tissues and cells, exerting their pharmacological aspects and alleviating a lot of diseased processes. Accordingly, this research is about introducing some isatins to be nucleophilically attacked at C3 forming products of azomethine ylide functionality. These iminium compounds were made by allowing certain isatins to be reacted with the secondary amino acid, proline, at acetic acid and methanol medium and then collected after purification to be identified with total Leukocyte count (TLC) and melting point. The structural characterization was performed by fourier-transform infrared spectroscopy (FTIR), proton nuclear magnetic resonance (1H-NMR), and community health nursing (CHN) analysis. The microbiological evaluatio
... Show MoreThe synthesis of complexes for (Ca+2, Co+2, Ni+2, Cu+2, Zn+2, Cd+2 and Hg+2) with new ligand (5-C-dimethyl malonyl-pentulose-γ-lactone-2,3-enedibenzoate) (L) have been successfully prepared and characterized by (1H and 13CNMR, FTIR, (U.V-Vis) spectroscopy, Atomic absorption spectrophotometer (A.A.s), Molar conductivity measurements and Magnetic moment measurements, and the following general formula has been given for the prepared complexes [M(L)Cl2] where M = (Ca+2, Co+2, Ni+2, Cu+2, Zn+2, Cd+2, Hg+2), L = (5-C-dimethyl malonyl-pentulose-γ-lactone-2,3-enedibenzoate).
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 MoreNew complcxcof Cu (ll),Ni(ll) ,Co(ll), and Zn(ll) wi th 2- amino-5-p-Fiouro Phenyl 1,3,4-Thiadiazole have been synthesized . The products were isolated , studied and characterized by physical measurements, i.e., (Ff -IR) ,UV-Vis and the melting points were determined .The new Schiff base (L) has been used to prepare some complexes .The prepared complexes were identified and their tructural geometry were suggested.