Etodolac 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 compared to etodolac.
A series of new imides compounds[1-4] were synthesized from reaction of tetrachlorophthalic anhydride or nitro phthalic anhydride or malic anhydride or Succinic anhydride with 4-amino benzene thiol under fusion conditions. Chloroacetic acid has been added after compounds [1-4] reacted with distilled H2O and Na2CO3, producing compounds [5-8]. In benzene, compounds [5-8] also interacted with the thionyl chloride to produce [9-12]. Poly (vinyl alcohol) was chemically modified by reacting PVA with compounds [9-12] and dimethyl formamide to produce compounds [13-16]. Iron oxide nanoparticles (IONPs) are mixed with modified PVA [13-16] to create nanocomposites [17-20]. Spectral and analytical data from synthesized compounds, such as 1
... Show MoreA series of new imides compounds[1-4] were synthesized from reaction of tetrachlorophthalic anhydride or nitro phthalic anhydride or malic anhydride or Succinic anhydride with 4-amino benzene thiol under fusion conditions. Chloroacetic acid has been added after compounds [1-4] reacted with distilled H2O and Na2CO3, producing compounds [5-8]. In benzene, compounds [5-8] also interacted with the thionyl chloride to produce [9-12]. Poly (vinyl alcohol) was chemically modified by reacting PVA with compounds [9-12] and dimethyl formamide to produce compounds [13-16]. Iron oxide nanoparticles (IONPs) are mixed with modified PVA [13-16] to create nanocomposites [17-20]. Spectral and analytical data from synthesized compounds, such as 1H-NMR, FTI
... Show MoreThe study was carried out in plant tissue culture laboratory, University of Baghdad during the period 2017-2019, as factorial experiment in complete randomized design, to study the effect of PEG at (0, 2, 4, 6 and 8%) on physiological and chemical changes in callus of three sunflower (Ishaqi 1, Aqmar and Al-haga) induced by the cultivation of the young stem in vitro under water stress. The content of callus cells of SOD, POD, CAT and APX enzymes as well as total dissolved carbohydrate were determined as indicators to determine the effect of PEG in callus tissue cells cultivated on medium equipped with the PEG concentrations. The results showed that cultivars were differs significantly, and A-haja variety was superior in increasing SOD to 12
... Show MoreObjectives: Six different Schiff bases were synthesized from ampicillin and amoxicillin with isatin, 5-bromoisatin, and 5-nitroisatin. Methods: Ampicillin and Amoxicillin are linked directly through their α-amino groups to the acyl side chain with isatin and isatin derivatives by nucleophilic addition using glacial acetic acid as a catalyst. Results: chemical structures of these Schiff bases were confirmed using FTIR, 1H NMR and elemental microanalysis. The antibacterial activity was evaluated by measuring minimum inhibitory concentration (MIC) values and showed various degrees of antibacterial activities when compared with parent drugs. Compounds 1a and 2b, which are the Schiff bases of ampicillin and amoxicillin with isatin, showed very
... Show MoreAim: The present study aims to improve the poor water solubility of zaltoprofen which is a non-steroidal anti-inflammatory drug (NSAIDs) with a potent analgesic effect using solid dispersion then formulate it as a hollow type suppository to be more convenient for geriatric patients. Materials and Method: Zaltoprofen solid dispersions were prepared by solvent evaporation technique in different zaltoprofen: Soluplus® ratios. Results: Among the formulations tested, zaltoprofen solid dispersion preparation using 1:5 (zaltoprofen: Soluplus®) ratio showed the highest solubility and selected for further investigation. Solid dispersion characterization was evaluated by differential scanning calorimetry (DSC), X-ray diffraction study (XRD) and Fou
... Show MoreThe study aimed to evaluate the antimicrobial activity using different concentrations of aqueous and alcoholic extracts of dried lemongrass leaves. Chemical phytochemical tests were performed for aqueous and alcoholic extracts of lemongrass. Antimicrobials activity was tested using agar disc diffusion method against Escherichia coli and Staphylococcus aureus. The results of the study showed that the aqueous extract of dried lemon leaves was highly effective (P≤0.05) against S. aureus, as the inhibition diameter was 22 mm for 50 dilution, while the inhibition diameter decreased to 15 mm for concentration 100. As for the alcoholic extract only, the diameter of inhibition decreased significantly (P≤0.0
... Show MoreThe purpose of this research is to prepare new vanillic acid derivatives with 1,2,4-triazole-3-thiol heterocyclic ring and evaluate their antimicrobial activity in a preliminary assessment. A multistep synthesis was established for the preparation of new vanillic acid-triazole conjugates. The intermediate of 4-(4-amino-5-mercapto-4H-1,2,4-triazol-3-yl)-2-methoxyphenol (4) reacts with different heterocyclic aldehydes (thiophene-2-carboxaldehyde, pyrrole-2-carboxaldehyde, thiophene-3-carboxaldehyde, and furfural ) in ethanol containing few drops of acetic acid yielded the corresponding 4-(4-(substituted amino)-5-mercapto-4H-1,2,4-1triazol-3-yl)-2-methoxy phenol derivatives (5-8). These compounds were characterized spectroscopically by
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