To 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 Naproxen in this regard. The synthesizedhydrazone of naproxen hydrazides with their pronounced anti-inflammatory activity can enhance the anti-inflammatory activity of naproxen to a varying degree according to the type of aldehyde or ketone used.
Abstract: New copper(II) complexes with mixed ligand benziloxime (BOxH) and furfural-dehydeazine (FA) using classical (with and without solvent) and microwave heating methods have been prepared. The resulting complexes have been characterized using physico-chemical techniques. The study suggested that the ligands formed neutral complexes had general formulas [Cu(FA)(BOXH)(Ac)2] and [Cu(FA)(BOX)(OH)] in neutral (or acidic) and basic medium, respectively. Accordingly, hexa-coordinated mono-nuclear complexes have been investigated by this study and having distorted octahedral geometry. The effect of laser have been studied on solid ligands and solid complexes, no effect have been observed on most compounds through the results of melting poin
... Show MoreBackground: Potentially malignant oral disorders (PMODs) are common precursors of oral squamous cell carcinoma (OSCC). Neoangiogenesis and signalling are important intermediate biomarkers that may govern the progression of dysplastic mucosa into carcinoma. Aims: Evaluate the importance of CD34 and Wnt3 expression in PMODs and OSCCs in relation to their clinicopathological parameters. Settings and Design: Prospective cross-sectional study. Materials and Methods: Immunohistochemical staining for CD34 and Wnt3 was performed for 41 samples. These included 27 PMODs, six OSCCs and eight normal gingival and alveolar mucosa. Analysis of variance (ANOVA) and post-hoc tests were applied. P<0.05 was considered statistically significant. Results: CD34
... Show MoreThe purpose of my thesis is to prepare four new ligands (L1-L4) that have been used to prepare a series of metal complexes by reacting them with metal ions: M=(Mn(II), Co(II), Ni(II), Cu(II), Zn(II), Cd(II), Hg(II) Where succinyl chloride was used as a raw material for the preparation of bi-dented ligands (L1-L4) by reacting it with potassium thiocyanate as a first step and then reacting with (2-aminobenzothiazole, Benzylamine, 4-aminoantipyrine, Sulfamethoxazole) respectively as a second step with the use of dry acetone as a solvent, the chemical formula of the four ligands prepared in succession: N1,N4-bis(benzo[d]thiazol-2-ylcarbamothioyl)succinamide (L1) N1,N4-bis(benzylcarbamothioyl)succinami
... Show MoreUnregulated epigenetic modifications, including histone acetylation/deacetylation mediated by histone acetyltransferases (HATs) and histone deacetylases (HDACs), contribute to cancer progression. HDACs, often overexpressed in cancer, downregulate tumor suppressor genes, making them crucial targets for treatment. This work aimed to develop non‐hydroxamate benzoic acid–based HDAC inhibitors (HDACi) with comparable effect to the currently four FDA‐approved HDACi, which are known for their poor solubility, poor distribution, and significant side effects. All compounds were structurally verified using FTIR, 1HNMR, 13CNMR, and mass spectrometry. In silico ana
In this paper, some series of new complexes of Mn(II), Co(II), Ni (II) Cu(II) and Hg(II) are prepared from the Schiff bases (L1,L2). (L1) derived from 4-aminoantipyrine and O-phenylene dia mine then (L2) derived from (L1) and 2-benzoyl benzoic acid. Structural features are obtained from their elemental microanalyses, molar conductance, IR, UV–Vis, 1H, 13CNMR spectra and magnetic susceptibility. The magnetic susceptibility and UV–Vis, IR spectral data of the ligand (L1) complexes get square–planar and tetrahedral geometries and the complexes oflig and (L2) get an octahedral geometry. Antimicrobial examinations show good results in the sharing complexes.
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 MoreIn this research, a new 1, 3, 4-Thiadiazole derivatives have been synthesized by many heterocyclic reactions. Starting from (2, 5 – dimercapto -1, 3, 4-Thiadiazole) a variety of derivatives have been synthesis. Compound (1) was synthesized by the reaction of hydrazine hydrate with carbon disulphide in absolute ethanol. The compound (1) was reacted with 1, 2-dibromoethane in presence of alkali ethanol to give the compound (2). The compound (3) was formed from the reaction of compound (2) with hydrazine hydrate. Schiff base (4) was obtained by reacting of compound (3) with the compound (p-hydroxybenzaldehyde) in absolute ethanol. A variety of phenolic Schiff base (Methylolic, Etheric, and Epoxy) derivatives have been synthesized. Methylol
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