This research includes the synthesis of some new different heterocyclic derivatives of 5-Bromoisatin. New sulfonylamide, diazine, oxazole, thiazole and 1,2,3-triazole derivatives of 5-Bromoisatin have been synthesized. The synthesis process started by the reaction of 5-Bromoisatin with different reagents to obtain schiff bases of 5-Bromoisatin intermediate compounds(1, 8, 19) by using glacial acetic acid as a catalyst in three routes. The first route, 5-Bromoisatin reacted with p-aminosulfonylchloride to product compound(1), then converted to sulfonyl amide derivatives(2-7) by the reaction of compound(1) with different substituted primary aromatic amine in absolute ethanol. The second route includes the reaction of 5-Bromoisatin rea
... Show MoreBackground: Hydatidosis is a widespread chronic zoonotic disease caused by helminthic larval stage of tapeworm Echinococcus granulosus. It has a serious medical and public health problem. Recently many substances are used to activate and modulate the immune system of the host in order to control the cyst growth and development.
Materials and Methods: Protoscolices were isolated from human hydatid cysts and treated with four purified concentrations (25, 50, 75, 100μm/ml) of 1-HP plus hydatid cyst fluid as a positive control group for 4, 24, 48 and 72 hrs period of exposure. Then After 72 hours, the protoscolices which were treated with different concentration of 1-HP were inoculated intraperitonially of m
Clotrimazole (CLO) is an antimycotic imidazole derivative applied locally for the treatment of vaginal yeast infections. In this study, CLO was formulated as vaginal mucoadhesive hydrogel, using different types of mucoadhesive polymers to ensure prolonged contact between active ingredient and vaginal mucosa.
Physicochemical properties of the prepared formulas were evaluated as a visual inspection, pH, swelling index, spreadability, and mucoadhesive characteristics, in addition to an in-vitro drug release. The influence of type and concentration of polymers as CMC-Na (1.5, 2.5, and 3.5%w/w), carbopol 940( 0.25, 0.5, and 1 %w/w) and poloxamer 407 (15, 25, 30%w/w) on CLO release from the prepared gels were also invest
... Show MoreLiquisolid compact is the most promising technique for increasing dissolution rate and bioavailability of poorly soluble drugs.Clopidogrel bisulfate is an oral antiplatelets used for treatment and prophylaxis of cardiovacular and peripheral vascular diseases related to platelets aggreagation.Clopidogrel has low solubility at high pH media of intestine and low bioavailability of a bout 50% after oral doses.The purpose of this work was to enhance dissolution pattern of clopidogrel through its formulation into liquisolid tablets.A mathematical model was used to calculate the optimum quantities of tween 80 , carrier (Avicel PH 102) and coating material (Aerosil 200) needed to prepare acceptably flowing and compactible powder mixtures.The liq
... Show MoreTo synthesize new hydrazone derivatives of naproxen with enhanced anti-inflammatory activity and devoid the ulcerogenic side effects. Hydrazones were synthesized by conjugation of naproxen hydrazide with seven natural and synthetic aldehyde and ketone by using glacial acetic acid as catalyst. The synthesis has been carried out following simple methodology in excellent isolated yields.The structure of the synthesized derivatives has been characterized by elemental microanalysis (CHN), FTIR Spectroscopy, and other physicochemical properties.The anti- inflammatory activity of the synthesized compounds was evaluated in vivo using the egg-white induced edema model in rats, and the results of the biological assay was found to be comparable to Nap
... Show MoreIn this work, combining acyclovir with ciprofloxacin (CCP), a new Schiff base and its metal complexes with iron (III), manganese (II), copper (II), zinc (II), and calcium (II) ions are synthesized and structurally characterized by XRD, SEM, 1H NMR, 13C NMR, FT-IR, and UV-Visible spectral techniques. Furthermore, molecular docking studies were carried out, and the complexes were tested to resolve any potential hang-ups in opposition to the Herpes virus and DFT calculation studies. In addition, the metal complexes and ligand were screened against antibacterial strains of one gram-positive bacteria (Staphylococcus aureus) and three gram-negative bacteria (
... Show MoreComplexes from the ligand (2-hydroxy benzaldine)-4-aminoantipyrine with some transition metal ions V(l?),Cr(lll),Fe(lll) and Co(ll) were prepared in the presence of the co-ligand 1,10-phenanthroline in alcoholic medium. These compounds were characterized by the available techniques: FT-IR ,UV-Visible ,magnetic susceptibility, Flame atomic absorption technique as well as elemental analysis and conductivity mesurments .From these spectral studies, a square pyramidal structure proposed for V(IV) complex and an octahedral geometry for Cr(III),Fe(III) and Co(II) complexes. The biological activity of the ligands and their complexes were evaluated by a gar plate diffusion technique against three human pathogenic bacterial strains: Pseudomonas ae
... Show MoreAbstract
Endophytic fungi are gaining interest as sources of novel bioactive metabolites.
The study was carried out to screen and isolate endophytic fungus.An endophytic
fungus isolated from root of calyptous plant .The fungus was identified as
Stemphylium radicinum (Meier, Drechs and Eddy)based on morphological
characterization. Fungal secondary metabolites was carried out by ethyl acetate
solvent.The antibacterial activity was tested against five bacterial isolates.
Esherichia coli, Staphylococcus aureus, Proteus vulgaris, Klebsiella pneumonia and
Streptococcus pyogenes by using a disc diffusion technique. The inhibition zones
exhibited by Fungal secondary metabolites were ranged between 22.5-35.5 mm.
Mini
Objective: Synthesized a series of new thiourea (TU) derivatives, tested their antioxidant activity, and investigated their expected biological activity by theoretical study (computational methods). Methods: The derivatives were made using a one-pot reaction with two steps. Initially, succinyl chloride was mixed with KSCN to make succinyl isothiocyanate. Then, primary and secondary amines were used to make TU derivatives. The theoretical studies were done by Swiss ADME and molecular docking via Genetic Optimization of Linkage Docking (GOLD). Then evaluate antioxidant activity using the DPPH scavenging method. Results: FT-IR, 1H NMR, and 13C NMR spectroscopy show the verification of all the prepared derivatives. Compounds (II), (VIII),
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