Objective(s): Biocompatibility, non-toxicity, minimal allergenicity, and biodegradability are all characteristics of chitosan. Other biological properties of chitosan have been reported, including antitumor, antimicrobial and antioxidant activities. This research aim is the synthesis of drug compounds by preparation and characterization of polymer chitosan Schiff base and chitosan Schiff base / Poly vinyl alcohol / poly vinyl pyrrolidone Nanocomposite and study applications (anticancer cell line, antimicrobial agents). Methods: Chitosan Schiff base was prepared from the reaction of chitosan with carbonyl group of 4-nitro benzaldehyde. Polymer blend have been prepared by solution casting method. Chitosan Schiff base mixing with PVA and PVP. Green synthesis of AuNPs and AgNPs by onion peals extract as reducing agent. Nanocomposites were prepared by mixing 10 mL of chitosan Schiff base, 5 mL PVA and 5 mL of PVP with 25 mL of two different concentrations (100, 200 ppm) of AuNPs and AgNPs. In vitro bacterial activities polymer blends and Au, Ag nano composites were performed against pathogenic bacteria such as the Acinetobacter baumannii, Staphylococcus aureus, Pseudomonas aeruginosa and Esherichia coli. Cancer cell line (AMJ-13) cell line. Results: The prepared AgNPs and AuNPs were characterized by UV-visible spectroscopy, SEM microscopy and XRD analysis. UV-vis spectrum of AuNPs at 543 nm and AgNPs at 425 nm, particles size of AuNPs 24.74 nm and AgNPs 18.77 nm. The polymer blends and nano composites were characterized by FT-IR, SEM, DSC and TGA. DSC analysis investigated the polymer blend and nano composites shows a good thermal stability for all prepared compounds. The inhibition zone of blend and nanocomposites The Inhibition zone of blend and Nano composites ranging between (8-15) millimetre with concentration of 20 mg. The inhibition rate of blend and Nanocomposites ranging between (1.33 – 77.33) for all compounds. IC 50 of blend and Nanocomposites ranging between (26.04 - 183.56) µg for all compounds. Conclusions: The prepared AgNPs and AuNPs were characterized by UV-visible spectroscopy, SEM microscopy and XRD analysis. UV-vis spectrum of AuNPs at 543 nm and AgNPs at 425 nm, particles size of AuNPs 24.74 nm and AgNPs 18.77 nm. The polymer blends and nano composites were characterized by FT-IR, SEM, DSC and TGA. DSC analysis investigated the polymer blend and nano composites shows a good thermal stability for all prepared compounds. The inhibition zone of blend and nanocomposites The Inhibition zone of blend and Nano composites ranging between (8-15) millimetre with concentration of 20 mg. The inhibition rate of blend and Nanocomposites ranging between (1.33 – 77.33) for all compounds. IC 50 of blend and Nanocomposites ranging between (26.04 - 183.56) µg for all compounds.
Amoxicillin 1 was treated with thiosemicarbazide and Phosphoryl chloride to obtain a new derivatives that contains 1,3,4-thiadiazole moiety 2. Schiff bases compounds were synthesized by the reaction of compound 2 with different aldehydes such as benzaldehyde and some substituted Benzaldehyde; p-hydroy, p-Chloro, p-Nitro, p-Dimethylamino, p-Methyl, p-Methoxy, p-Ethoxy to give compounds 3a-h. The obtained compounds have tested towards gram -ve and gram +ve bacteria. The compound shows good to moderate result towards the bacteria.
The systemic and resistant nature of metastatic castration-resistant prostate cancers (mCRPC) renders it largely incurable even after intensive multimodal therapy. Proliferation, survival, and epithelial-mesenchymal transition (EMT) are three fundamental events that are deeply linked to carcinogenesis. Hence, it is necessary to find a new combination of several therapies, targeting those vital mechanisms without causing side effects. Significant research works have shown differential low expression of the metabolic Farnesoid X receptor (FXR) in primary and metastatic prostate cancer suggesting their importance in prostate pathogenesis. Obticholic acid (INT 747), a potent FXR agonist is widely used in primary biliary chola
... Show MoreNew Schiff base [3-(3-acetylthioureido)pyrazine-2-carboxylic acid][L] has been prepared through 2 stages, the chloro acetyl chloride has been reacting with the ammonium thiocyanate in the initial phase for producing precursor [A], after that [A] has been reacting with the 3-amino pyrazine-2-carboxilic acid to provide a novel bidentate ligand [L], such ligand [L] has been reacting with certain metal ions in the Mn(II), VO(II), Ni(II), Co(II), Zn(II), Cu(II), Hg(II), and Cd(II) for providing series of new metal complexes regarding general molecular formula [M(L)2XY], in which; VO(II); X=SO4,Y=0, Co(II), Mn(II), Cu(II), Ni(II), Cd(II), Zn(II), and Hg(II); Y=Cl, X=Cl. Also, all the compounds were characterized through spectroscopic techniques [
... Show MoreNew derivatives of the anti-inflammatory, leprostatic drug dapsone 4 are synthesized, characterized and biologically screened by the treating the drug dapsone with chloroacetyl chloride in the presence of base. Both amino groups are acylated to give compound 6. The symmetrical acylated product then treated with Phenol, N-Acetyl-p-aminophenol, p-Chlorophenol, m-Chlorophenol, o-Hydroxybezoic acid and m-Hydroxybezoic acid to give compounds 8(a-f). The antimicrobial activity was tested for the synthesized compounds; activates were good compared to the parent drug. All the new compounds have scanned for their biological activities toward gram ‒ve and gram +ve (M. tuberculosis, S. pneumoniae, E. coli and P. mirabilis) bacteria, the synthesized
... Show MoreA new series of N-acyl hydrazones (4a-g) derived from indole-3-propionic acid (IPA) were synthesized. These N-acyl hydrazones were prepared by the reaction of 3-(1H-indol-3-yl) propane hydrazide and aldehyde in the existence of glacial acetic acid as a catalyst. 1HNMR and FT-IR analyses were used to identify the synthesized compounds and they were in vitro evaluated as antibacterial agents against six different types of microorganisms by using well diffusion method. All the tested N-acyl hydrazones (4a-g) displayed moderate activity against the Gram-negative E.coli, comparable to that of Amoxicillin. Some of the tested N-acyl hydrazones also exhibited intermediate activity ag
... Show MoreThree of imide intermediate products were synthesized by reacting of phthalic anhydride with glycine (2a), and tetrachloro phthalic anhydride with glycine , (S)-2-[(tert-Butoxycarbonyl)amino]-3-aminopropionic acid ( 2b,c) respectively in dry toluene with azeotropic removal of water using Dean- stark apparatus then carboxyl functional group activated by refluxing with thionyl chloride, the resulted acid chloride (3a-c) were reacted with different amine (5-flourouracil, 4-chloroaniline, 4-bromoaniline, 2-amino thiazole, and pyrrolidine) (4a-e) , the resulted products consider as
... Show MoreThe green production of iron oxide nanoparticles (FeONPs) due to its numerous biotechnological uses has attracted a lot of attention and clean and eco-friendly approaches in the medical field.
The objectives of this study are to demonstrate the biogenic creation of FeONPs. The search for alternative antimicrobial medicines has been prompted by growing worries about multidrug resistance.