This work has been done to prepare a series of new alkene compounds derived from 4-thiozolidinones by substituting different aldehydes, P-acetamido-phenol, and 2-mercapto-benzoimidazole, which were used as starting materials to form ester [I]a,b and then make hydrazides [II]a,b, which were used to prepare 1, 3, and 4-oxadiazoles [III]a,b, which were then used for prepared Schiff bases [IV]a-f, The next step was the synthesis of 4-thiazoldinone derivatives [V]a-f from Schiff bases. The final step was the synthesis of alkenes [VII]a-f, the prepared derivatives were identified with spectral methods (FT-IR, 1H-NMR, mass, and CHNS). The antibacterial activity of the prepared derivatives was evaluated against four types of bacteria, positive gram (Staphylococcus aureus and Enterococcus faecalis.) and negative gram (E. coli and Pseudomonas aerugionsa). The final compounds gave high to moderate efficacy against Enterococcus faecalis bacteria, molecular modeling study against one of the SARS human coronavirus proteins was tested for synthesis compounds. Compound [VII]c had a high bonding strength with the target protein, wherever it was -8.08 Kcal/mole followed by the compound [VII]a. in the bonding strength energy, which was -7.65Kcal/mole.
Lafutidine (LAF) a newly developed histamine H2-receptor antagonist with absorption window makes it a good candidate to be prepared as floating drug delivery system. The current study involves formulation and in- Vitro evaluation of lafutidine as floating microspheres. Different formulation variables that affect the physicochemical properties of the prepared microspheres besides to the drug release behavior were investigated. Fourteen formulas were prepared by emulsion (o/w) solvent evaporation method using Ethyl cellulose (EC) as the polymeric matrix and tween 80 (TW80) as an emulsifying agent. The prepared formulas were evaluated for their percentage buoyancy (%), Percentage yield (%) and Entrapment efficiency (EE %). The results obt
... Show MoreIn this work, we introduce a new kind of perfect mappings, namely j-perfect mappings and j-ω-perfect mappings. Furthermore we devoted to study the relationship between j-perfect mappings and j-ω-perfect mappings. Finally, certain theorems and characterization concerning these concepts are studied; j = , δ, α, pre, b, β
The Fylex extract exert a high inhibition effect against A . flavus growth on PDA medium, as the fungus growth was completely inhibited by 100% at a concentration of 0.2 and 0.3% of studied extract, while the lowest inhibition percentage (71%) was found at a concentration of 0.1%. Whereas magnesium oxide nanoparticles showed the highest inhibition ratio of A. flavus (100%) was detected at 0.2% and the lowest inhibition ratio (81.66%) was at concentration 0.5%. Moreover, the addition of G. lucidum powder to PDA medium with a concentration of 2.5 mg increased the inhibition rate of A. flavus growth which was 54.4%, while the lowest inhibition ration (18.22%) was found at a concentration of 1000 mg. The milky liquid (brocade milk) of Calotropi
... Show MoreA variety of liquid crystals comprising heterocyclics 1,3,4-oxadiazol ring [III], aminooxazol [IV]a, and aminothiazol [IV]b were synthesized through a number of steps, beginning of the reaction of 3, 3'- dimethyl - [1, 1'-biphenyl] -4, 4'- diamin, ethyl monochloroacetate and sodium acetate to synthesize diacetate compound[I]. The diester reacted with hydrazine hydrate(N2H4-H2O) to give dihydrazide compound [II], then reacted with Pyruvic acid and phosphorous oxychloride to produce diketone compound [III]. The last compound was reacted with urea and thiourea to give aminooxazol and aminothiazol respectively. The synthesized compounds actually characterized and determined the structures by melting points, FT-IR and 1H-NMR spectroscopies. By u
... Show MoreThis work includes two steps of synthesis, the first one is the synthesis of indole which was prepared according to literature of the reaction of phenyl hydrazine with acetaldehyde in glacial acetic acid afforded phenyl hydrazone of acetaldehyde , this product was fused with zinc chloride to give the indole.Reaction of cyclohexanone with phenyl hydrazine using the same procedure for the preparing giving 1,2,3,4-Tetrahydrocarbazole.Second step involved synthesis of a series of (17) of mannich bases derivatives of indole and 1,2,3,4-Tetrahydrocarbazle. Mannich reaction involves the condensation of aldehyde usually formaldehyde with different secondary amine and with compound containing an activated hydrogen.The reaction illustrated by the fo
... Show MorePropranolol is a nonselective-adrenergic blocker used in the treatment of hypertension, cardiac arrhythmias, and angina pectoris. A significant problem in propranolol therapy is that it undergoes extensive presystemic metabolism after oral administration leading to reduced bioavailability. In this study, two new propranolol derivatives have been designed, synthesized and characterized. These compounds were formed by acylation of propranolol followed by nucleophilic substitution reaction of acylated propranolol, these derivatives were analyzed for IR, CHN, melting points, and evaluated for their lipophilic properties compared with propranolol. The lower partition coefficient of these two derivatives revealed that the prodrug approach may be
... Show MoreIsolation of fungi was performed from February to July, 2019. One hundred clinical specimens were collected from King Abdullah Hospital (KAH) Bisha, Saudi Arabia. Samples were collected from twenty patients of different ages (30 - 70 years old) ten males and ten females. The samples were collected from patients with the two types of diabetics. Specimens included blood, hair, nail, oral swabs and skin. Specimens were inoculated on Sabourauds Dextrose agar containing chloramphenicol. Thirteen fungal species were isolated and identified. The isolated species were: Aspergillus flavus, A. niger, A. terrus, A. nidulans, A. fumigatus, Candida albicans, C. krusei, C. parapsilosis, C. Tropicalis, Curvularia lunata, Fusarium solani, Penicill
... Show MoreThe aim of this work is synthesis of _Eoly (Vinyl-4-AminoBenzoate) (PVAB) from reaction of _Eoly Vinyl Alkohol PVA with 4-aminobenzoyl chloride in alkaline media. We also prepare the metal complexes of poly (vinyl- 4-aminobenzoate) and antimicrobial properties were evaluated by dilute method against five pathogenic bacteria (Escherichia coli, Shigella dysentery, Klebsiella pneumonae, Staphylococcus aureus, Staphylococcus Albus) and two fungal (Aspergillus Niger, Yeast). All polymer metal complexes showed different activities against the various microbial isolates. The polymer metal complexes showed higher activity than the free polymer.
N-Benzylidene m-nitrobenzeneamines (Schiff bases) were prepared by condensation of m-nitroaniline with aromatic aldehydes. These Schiff bases were found to react with maleic anhydride to give 2-Aryl-3-(m-nitrophenyl)-2, 3-dihydro [1, 3] oxazepine–4, 7–diones and with phthalic anhydride to give 2-Aryl-3–(m-nitrophenyl)–2, 3–dihydrobenz|| 1, 2-e|||| 1, 3] oxazepine–4, 7-diones which were reacted with pyrrolidine to give the anilide–pyrrolidides of maleic acid and phthalic acid.