The purpose of this research work is to synthesize conjugates of some NSAIDs with sulfamethoxazole as possible mutual prodrugs to overcome the local gastric irritation of NSAID with free carboxyl group by formation of ester linkage that supposed to remain intact in stomach and may hydrolyze in intestine chemically or enzymatically; in addition to that attempting to target the synthesized derivative to the colon by formation of azo group that undergo reduction only by colonic bacterial azo reductaze enzyme to liberate the parent compound to act locally (treatment of inflammation and infections in colon)
Bacterial infections pose an ongoing challenge due to resistance developed by infectious bacteria. So much research targeting designing new antibacterials is published annually. Our goal is to synthesize compounds that have given antibacterial activity according to molecular docking against the chosen target protein and that have acceptable ADMET properties that can be synthesized and used in the future. New 2-(5-methoxy-1-(4-chlorobenzene)-2-methyl-1H-indol-3-yl)acetohydrazide derivatives’ antibacterial efficacy against two common strains of Gram-negative and Gram-positive microorganisms has been developed, produced, and investigated. Sophisticated, modern analytical methods, including ATR-FTIR and 1H NMR spectroscopy, were used
... Show MoreA group of amine derivatives [4-aminobenzenesulfonamide derivatives, 2-aminopyridine and 2-aminothiazole] incorporated to α-carbon of diclofenac a well known non-steroidal anti-inflammatory drug (NSAID) to increase bulkiness were designed and synthesized for evaluation as a potential anti-inflammatory agents with expected COX-2 selectivity. In vivo acute anti-inflammatory activity of the selected final compounds (9, 12 and 13) was evaluated in rats using egg-white induced edema model of inflammation in a dose equivalent to (3 mg/Kg) of diclofenac sodium. All tested compounds produced a significant reduction in paw edema with respect to the effect of propylene glycol 50
... Show MoreIn this study, a bioadhesive dosage form of eoconazole nitrate for vaginal delivery was designed using a combination of bioadhesive polymers: Carbopol 941 p and sodium carboxymethylcellulose or methylcellulose in different ratios. The bioadhesive strength was evaluated by measuring the force required to detach the tablet from sheep vaginal mucosal membrane. It was found that the bioadhesive force was directly proportional to Carbopol 941 p content in the different formulae. The formulae were tested for their swelling behavior using agar gel plate method. The results showed that formulae containing a combination of Carbopol 941 p and sodium carboxymethylcellulose had greater swelling index
... Show MoreThe drug promethazine hydrochloride (PRZH) forms with rhodium (II) a colored chelate (?max = 472 nm) complex at (pH = 2.1) which is extractable with benzyl alcohol as organic solvent. Under the appropriate experimental conditions a calibration plot was set up from which some analytical parameter were derived and deduced by regression. Standard addition procedure was also adopted. It has been estimated that the concentration of the drug PRZH to be 24.89 mg per unit and 24.19 mg per unit for both calibrations. Under optimal conditions, the developed method has been achieved the following characteristics: LDR (30 – 150 µg ml-1 ) PRZH , RSD % ( 0.6 – 2.47 ) , sandell sensitivity( 0.0844 µg. cm -2 ) , LOD ( 1.66 µgml-1 ) , recovery
... Show MoreChloroacetamide derivatives (2a-g) have been prepared through reaction of chloroacetyl chloride(1) (which prepared by the reaction of chloroacetic acid with thionyl chloride) with primary aromatic amines and sulfa compounds to afford compounds (2a-g) which then reacted with p-hydroxy benzaldehyde via Williamson reaction to obtaine the new compounds 2-(4-formyl phenoxy)-N-aryl acetamide (3a-g). Finally , compounds (3a-g) will be use as a good synthon to prepare the Schiff bases represented by compounds 2-(4-aryliminophenoxy)-N-arylacetamide (4a-g). through , reaction with some primary aromatic amine. All the prepared compounds were investigated by the available physical and spectroscopic methods.
Four novel Schiff bases SB1 to SB4 as new aromatic compound not hydrolysed under ordinary conditions were synthesized in this study by condensation reactions between2,4dinitrophenylhydrazine: firstly with 2,4,4`-trihydroxybenzophenone to give SB1, secondly with 4hydroxybenzophenone to give SB2, thirdly with 4-dimethylaminobenzaldhyde to give SB3 and fourthly with 4-aminobenzaldehyde to give SB4. The molecular structures of these aromatic Schiff bases obtained were identified and characterized based on melting points, elemental analysis(CHN), FT-IR and UV-Visible spectra. The electronic absorption spectra of Schiff bases obtained were studied in the solvents of ethanol, DMF, water, chloroform, carbon tetrachloride and cyclohe
... Show MoreThis search include the synthesis of some new 1,3-oxazepine derivatives have been prepared, starting from reaction of L-ascorbic acid with dry acetone in presence of dry hydrogen chloride afforded the acetal (I). Treatment of the latter with p-nitrobenzoyl chloride in pyridine yielded the ester (II) which was dissolved in (65%) acetic acid in absolute ethanol yielded the glycol (III). The reaction of the glycol (III) with sodium periodate in distilled water at room temperature produced the aldehyde (IV). The compound (V) [4-(1,3-dioxoisoindolin-2-yl)benzoic acid] was synthesized by reaction p-aminobenzoic acid and phthalic anhydride in presence of (gla. CH3COOH). Reaction of compound (V) with thionyl chloride produced [4-(1,3-dioxoisoindoli
... Show MoreThe preparation, spectroscopic characterisation of complexes derived from the mixed ligands with CdII, ZnII and CoII metal ions with Schiff base, Dithiocarbamates (DTCs) and 8-Hydroxyquinoline are reported. The compounds that prepared have been defined via; chloride content, F.T-IR, UV-Vis 1H-NMR spectroscopy and C.H.N.S, as well as conductance and magnetic susceptibility.All data which collected from such methods specified complexes with 6 coordinates in solution and solid states. The biologicalactivity that is related to all the prepared compounds which were screened for their antimicrobial activitiesagainst (G+ and (G- )). The data that collected from biological activity indicate that complexes will have extra activity against such teste
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