2-hydrazinylbenzo[d]thiazole compound [1] is produced from reaction of 2-mercapto-benzothiazole with hydrazine hydride in ethanol. Compound [1] reacted with maleic anhydride in DMF to produce (Z)-4-(2-(benzo[d] thiazol-2yl) hydrazinyl)-4-oxobut-2-enoic acid [compound (2)]. While the treatment of compound [2] with the ammonium persulfate (NH4)2S2O8 (as the initiator) in order to produce compound [3], then compound [3] reacted with thionyl chloride in benzene to produce compound [4], finally compound [4] reaction with various drugs: cephalexin, amoxicillin, sulfamethizole, elecoxib obtained polymers [5–8]. The structure of synthesized compounds identified by spectral data: fourier transform infrared (FTIR) and proton nuclear magnetic resonance (1HNMR) spectroscopy. The polymers [5–8] have been screened for their antibacterial activities against Staphylococcus aureus (G+), Escherichia coli (G-) and compared with the drug (amoxicillin). The anticancer activity (Hep G2 (human liver cancer cell line) of some prepared polymers were also studied.
Meloxicam (MLX) is non-steroidal anti -inflammatory, poorly water soluble, highly permeable drug and the rate of its oral absorption is often controlled by the dissolution rate in the gastrointestinal tract. Solid dispersion (SD) is an effective technique for enhancing the solubility and dissolution rate of such drug.
The present study aims to enhance the solubility and the dissolution rate of MLX by SD technique by solvent evaporation method using sodium alginate (SA), hyaluronic acid (HA), collagen and xyloglucan (XG) as gastro-protective hydrophilic natural polymers.
Twelve formulas were prepared in different drug: polymer ratios and evaluated for their, percentage yield, drug content, water so
... Show MoreHighly Modified Asphalt (HiMA) binders have garnered significant attention due to their superior resistance to rutting, fatigue cracking, and thermal distress under heavy traffic loads and extreme environmental conditions. While elastomeric polymers such as Styrene- Butadiene-Styrene (SBS) have been extensively used in HiMA applications, the potential of plastomeric polymers, including Polyethylene (PE) and Ethylene Vinyl Acetate (EVA), remains largely unexplored. This study aims to evaluate the performance of reference binder (RB) modified with plastomeric HiMA asphalt in comparison to SBS-modified binders and determine the optimal polymer dosage for achieving an optimal balance between rutting resistance and fatigue durability. The experi
... Show MoreThis study was performd on 50 urine specimens of patients with type 2 diabetes, in addition, 50 normal specimens were investigated as control group. The activity rate of maltase in patients (6.40±2.17) I.U/ml and activity rate of maltase in normal (0.44±0.20)I.U/ml. The results of the study reveal that maltase activity of type 2 diabetes patient's urine shows significant increase (P<0.01) compare to normal.
Aspartate aminotransferase was purified from urine and serum of patients with type 2 diabetes in a 2 steps procedure involving dialysis bag and sephadex G-25 gel filtration (column chromatography). The enzyme was purified 346.23 fold with 1467% yield and 3.46 fold with 142.85% yield in urine and serum of patients with type 2 diabetes respectively. The purified enzyme showed single peak. The results of this study revealed that AST activity of type 2 diabetes urine and serum increased significantly (p<0.001) compared with control group.
Novel derivatives of 1-(´1, ´3, ´4, ´6-tetra benzoyl-β-D-fructofuranosyl)-1H- benzotriazole and 1-(´1, ´3, ´4, ´6-tetra benzoyl-β-D-fructofuranosyl)-1H- benzotriazole carrying Schiff bases moiety were synthesised and fully characterised. The protection of D- fructose using benzoyl chloride was synthesized, followed by nucleophilic addition/elimination between benzotria- zole and chloroacetyl chloride to give 1-(1- chloroacetyl)- 1H-benzotriazole. The next step was condensation reaction of protected fructose and 1-(1-chloroacetyl)-1H- benzotriazole producing a new nucleoside analogue. The novel nucleoside analogues underwent a second conden- sation reaction with different aromatic and aliphatic amines to provide new Schiff b
... Show MoreDespite extensive investigation as biocompatible drug carriers, gelatin nanoparticles (GNPs) have not been thoroughly assessed for carrying chemically distinct cationic molecules such as acriflavine (ACF) and triethylenetetramine (TETA). In this study, we hypothesize that GNPs can effectively encapsulate ACF and TETA, forming stable delivery systems with distinct antibacterial and cytotoxic activities. ACF encapsulated in gelatin was prepared adapting desolvation technique. The procedure involved stirring of an aqueous solution of gelatin and ACF at room temperature, the pH was titrated to eight using NaOH followed by addition of ethanol. The resulting nanopart
A new ligand [N-(4-nitrobenzoylamino)-thioxomethyl] phenylalanine is synthesized by reaction of 4-nitrobenzoyl 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(NBA)2] where M2+ = Mn, Co, Ni, Cu, Zn, Pd, Cd and Hg, the proposed molecular structure for these complexes as tetrahedral geometry, except copper and palladium complexes are have square planer geometry.
A new ligand [N-(3-acetylphenylcarbamothioyl)-4-chlorobenzamide] (CAD) was synthesized by reaction of 4-Chlorobenzoyl isothiocyanate with 3-amino acetophenone, The ligand was characterized by elemental micro analysis C.H.N. S., FT-IR, UV-Vis and 1H,13C- NMR spectra, some transition metals complexes of this ligand were prepared and characterized by FT-IR, UV-Vis spectra, conductivity measurements, magnetic susceptibility and atomic absorption, From obtained results the molecular formula of all prepared complexes were [M(CAD)2(H2O)2]Cl2 (M+2 =Mn, Co, Ni, Cu, Zn, Cd and Hg),the proposed geometrical structure for all complexes were octahedral.
A group of amine derivatives [4-aminobenzenesulfonamide derivatives, 2-aminopyridine and 2-aminothiazole] incorporated to α-carbon of diclofenac a well known non-steroidal anti-inflammatory drug (NSAID) to increase bulkiness were designed and synthesized for evaluation as a potential anti-inflammatory agents with expected COX-2 selectivity. In vivo acute anti-inflammatory activity of the selected final compounds (9, 12 and 13) was evaluated in rats using egg-white induced edema model of inflammation in a dose equivalent to (3 mg/Kg) of diclofenac sodium. All tested compounds produced a significant reduction in paw edema with respect to the effect of propylene glycol 50
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