The work involves synthesis of new Schiff bases ([V] a, b and [VI] a, b), pyrazoles [VII] a, b and pyrazolines [VIII] a, b derivatives containing isoxazoline unit starting with chalcones. 4-bromoacetophenone was reacted with 4-hydroxybenzaldehyde or 4-hydroxyacetophenone was reacted with 4-bromobenzaldehyde in basic medium to give chalcone by Claisen-Schemidt reaction. The chalcons [I] a, b was reacted with hydroxylamine hydrochloride to form isoxazolines [II] a, b. which were reacted with ethyl chloro acetate in basic medium to get ester compounds [III] a, b. The condensation new ester [III] a, b with hydrazine hydrate80% yieldedacid hydrazide [IV] a, b. The later compound refluxing with 4-substituted benzaldehyde in dry benzene to give Schiff bases ([V] a, band [VI] a, b) while the reaction of acid hydrazide [IV] a, b with acetylacetone or ethyl aceto acetate to get pyrazole [VII] a, b, pyrazolone [VIII] a, b, respectively. The synthesized compounds were characterized by melting points, FTIR, mass and 1H NMR spectroscopy
The present investigation developed the ester prodrugs of Non-steroidal anti inflammatory drugs (NSAIDs), Mefenamic acid and Flurbiprofen by conjugating with the natural antioxidant, 4-methyl umbelliferone that resulted the formation of Mefenamic acid-umbelliferone ester prodrug and Flurbiprofen-umbelliferone ester prodrug .The principal objective this study is the synthesis of the ester prodrugs of NSAIDs with the enhanced therapeutic activity and minimized side effects. Prodrugs were synthesized by coupling method using N,N’- dicyclohexylcarbodiimide/4-dimethylaminopyrimidine, subjected to physical, chemical characterization, spectral characterization (IR, 1H NMR, 13C NMR and Mass spectra),hydro
... Show MoreEtodolac is choice of drug for pain and inflammation but has major side effects of gastric ulcers that are due to free carboxylic group. Etodolac belongs to the chemical class of non-selective COX-inhibitor but preferentially COX-2 inhibitor. Here the ester linked mutual prodrugs of etodolac with phytophenols like vanillin, carvacrol, umbelliferone, guaiacol, sesamol and syringaldehyde were synthesized. All the prodrugs were characterized by IR-spectroscopy, 1H-NMR, 13C-NMR and mass spectrometry. Among the synthesized prodrugs, the Eto-van, Eto-umbe, Eto-sesa and Eto-syr showed improved analgesic and anti-inflammatory activity compared to etodolac. All the synthesized prodrugs showed less ulcerogenic side effects co
... Show MorePorous Silicon (PS) layer has been prepared from p-type silicon by electrochemical etching method. The morphology properties of PS samples that prepared with different current density has been study using atom force measurement (AFM) and it show that the Layer of pore has sponge like stricture and the average pore diameter of PS layer increase with etching current density increase .The x-ray diffraction (XRD) pattern indicated the nanocrystaline of the sample. Reflectivity of the sample surface is decrease when etching current density increases because of porosity increase on surface of sample. The photolumenses (PL) intensity increase with increase etching current density. The PL is affected by relative humidity (RH) level so we can use
... Show MoreAlthough the number of implants has increased gradually and consistently over the years to around one million per year globally, there is still far more potential for advancement in the field of dental implantology which is typically growing quickly. This study investigates the effect of nanofiller reinforcement high-performance polymer matrix to enhance mechanical and physical characteristics. Calcium silicate (CS)/Polyetherketoneketone (PEKK) biomedical composite (G0 as a control group) is reinforced with different weight percentages (G1-G4) of tellurium dioxide nanoparticles (TeO2NPs) ( n = 5). This research uses ethanol as a binder for mixing various weight percentages (wt%) of TeO2NPs w
... Show MoreLetrozole (LZL) is a non-steroidal competitive aromatase enzyme system inhibitor. The aim of this study is to improve the permeation of LZL through the skin by preparing as nanoemulsion using various numbers of oils, surfactants and co-surfactant with deionized water. Based on solubility studies, mixtures of oleic acid oil and tween 80/ transcutol p as surfactant/co-surfactant (Smix) in different percentages were used to prepare nanoemulsions (NS). Therefore, 9 formulae of (o/w) LZL NS were formulated, then pseudo-ternary phase diagram was used as a useful tool to evaluate the NS domain at Smix ratios: 1:1, 2:1 and 3:1.