Non-steroidal anti-inflammatory drugs (NSAIDs) contain free –COOH which thought to be responsible for the GI irritation associated with all traditional NSAIDs. The esterification of this group is one of an approach to ultimate aim for reduce the gastric irritation; so in this study we synthesized and preliminarily evaluated new ester compounds as new analogues with expected selectivity toward COX-2 enzyme. Synthetic procedures have been successfully developed for the generation of the target compounds (III a and b). The synthetic approach involved multi-steps procedures which include: Synthesis of 4-hydroxy benzene sulphonamide ( I b ), synthesis of Naproxen and Ibuprofen acyl chloride and then reacting them with 4-hydroxy benzene sulphonamide to form final compounds ( III a-b) .The structures of these compounds were identified and characterized using (TLC), infrared spectroscopy (FT-IR), 1H NMR data and microanalysis (CHN).Pharmacological study as anti-inflammatory activities for the final compounds were studied in rats by induced edema type of inflammation. Moreover, the results of a docking study of compounds III a-b into the COX-2 binding site revealed that its mechanism was possibly similar to that of naproxen, a COX-2 inhibitor. The effect of them on COX-2 antibody was showed it could significantly inhibit COX-2 activity.
Leishmania parasites are the causative agent of leishmaniasis. Many studies are inspecting chemical drugs, including the use of miltefosine and amphotericin B, but curative values may be limited for these drugs with side effects due to the chemical origin, therefore, investigating less toxic therapies is essential. The aim of this study was to investigate the effectiveness of artemisinin on Iraqi strain of Leishmania tropica, by experimental macrophage ex vivo infection of amastigotes into mouse macrophage cell-line RAW264.7. Different concentrations (100, 200, 300, 400, 500)μM of artemisinin (ART) were screened to examine the susceptibility of L. tropica amastigotes to invade macrophage cell line along three times of follow up (24, 48 and
... Show MoreHeterocyclic compounds are employed in many applications, and numerous researchers have created liquid crystals by adding heterocyclic to the structures of these molecules. This work includes the synthesis and characterization of new compounds that contain 5H-thiazolo [4,3-b][1,3,4] thiadiazol united in multiple steps, starting with the synthesis of the aldehyde compound [I] by reaction chloro ethyl acetate with 4-hydroxybenzaldehyde in the presence of ethanol and potassium carbonate, followed by reactions with thiosemicarbazide, mercapto acetic acid in sulphuric acid to produce compound [II] then reflux compound [II] with hydrazine hydrate to product compound [III], after that reaction the later compound with nalkoxybenzaldehyde [IV]n and
... Show MoreNew thermally stable aromatic poly(amide-imide)s ( PAI1- PAI4 ) were synthesized from direct polycondensation reaction of Terephthalic acid and Phthalic acid with two new different diamine monomers derivatives of 1,2,4,5-tetracarboxilic benzene dianhydride as a second diacides in a medium consisting of triphenyl phosphite (TPP) in N-methyl-2pyrrolidone (NMP) / pyridine solution containing dissolved calcium chloride CaCl2. The polymerization reaction produced a series of novel poly(amide-imide) in high yield. The new monomers were characterized by FTIR, 1H-NMR spectroscopy. The resulting polymers were typically characterized by means of FT-IR, 1H-NMR spectroscopy, and solubility tests. Thermal properties of the poly(amide-imide)s were als
... Show MoreIsolation had been done for active substances from Thyme plant (Thymus Vulgaris) such as volatile oils, Saponins and Tannins. The percentage in form was (21.1%),(59.2%),( 9.7%) respectively. Also a study of anti-bacterial activity of extracts from Thyme using two types of pathogenic bacteria Escherichia Coli and aurous Staphylococcus showed the ability of inhibition for all different extracts by vary inhibition diameters for different active substances, concentrations and bacteria. One type of cancer cellular line used to study the effect of Thyme extracts on the growth of cells in the laboratory and thus know the specifications of extracts as anti-tumor, (L20B) cell line have been used which is mice Transformed cell Line. The possibility o
... Show MoreTHE Schiff base reaction played an important role of the condensation reaction between 2-aminophenol and Glyoxylic acid in the presence of calculated amounts of KOH as a catalyst. The reaction has been carried out in ethanol under reflux and stirring condition for 3.5 hrs. All syntheses were carried out under hydrogen gas forming a new potassium (E)-1-hydroxy-2-(2-hydroxyphenylimino)ethanolate ligand type [NO2]. The ligand of the general formula K2[Mn(L2)] type and its Mnп complex K2[Mn(N2O4)] type, has been characterized by spectroscopic methods (F.T-I.R. and U.V-Vis.), elemental analysis (C.H.N) metal content, magnetic susceptibility measurement, Thin-layer chromatography (T.L.C), X-RD powder diffraction, 1H-NMR, 13C-NMR molar conductanc
... Show MoreA new Schiff base ligand [L] [3-methyl-9,10 phenyl -6,7 dihydro-5,8 –dioxo-1,2 diazo –cyclo dodecu 2,11-diene ,4-one ] and its complexes with (Co(II), Ni(II), Cu (II), Zn(II) and Cd(II)) were synthesis.This ligand was prepared in three steps, in the first step a solution of salicyladehyed in methanol reacted under refluxed with hydrazine monohydrate to give an (intermediate compound 1) which reacted in the second step with sodium pyruvate to give an (intermediate compound 2) which gave the ligand [L] in the three step when it reacted with 1,2- dichloro ethane.The complexes were synthesized by direct reaction of the corresponding metal chloride with the ligand. The ligand and complexes were characterized by spectroscopic methods [IR, UV-
... Show MoreThe increasing anti-bacterial drug resistance is one of the biggest challenges facing doctors around the globe, so finding alternative treatments is one of the ideal options to overcome this problem. The cruciferous family is one of the wealthiest plants worldwide because it contains the most important secondary metabolites, glucosinolates, known for their anti-microbial properties. The present study aimed to evaluate the anti-bacterial effect of glucosinolates (Sinigrin) against eight bacterial isolates (Staphylococcus aureus, Enterococcus faecalis, Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa, Actinomyces, Proteus mirabilis and Streptococcus pneumoniae). The current study investigated six concentrations of pure
... Show MoreBackground In recent years, there has been a notable increase in the level of attention devoted to exploring capabilities of nanoparticles, specifically gold nanoparticles AuNPs, within context of modern times. AuNPs possess distinct biophysical properties, as a novel avenue as an antibacterial agent targeting Streptococcus Mutans and Candida Albicans. The aim of this study to create a nano-platform that has the potential to be environmentally sustainable, in addition to exhibiting exceptional antimicrobial properties against Streptococcus Mutans as well as Candida Albicans. Methods this study involved utilization of
Heterocyclic polymers / silica nanocomposite one of important materials because of excellent properties such as thermal , electrical , and mechanical properties , so that hybrid nanomaterial are widely used in many fields, in this paper nanocomposite had prepared by modification of silica nanoparticals by using acrylic acid and functionalized the surface of nanoparticles, and using free Radical polymerization by AIBN as initiators and anhydrous toluene as solvent to polymerize functionalize silica nanoparticles with heterocyclic monomers to prepare heterocylic polymers / silica nanocomposite and study electrical conductivity , The nanocomposite which had prepared characterized by many analysis technique to study thermal properties such
... Show MoreThis work include synthesized and characterization the compound [I] by reaction 1,4-phenylenediamine with chloro acetic acid then this compound reaction with methanol in present sulfuric acid to synthesized ester compound [II] after that reaction with hydrazine hydrate to synthesized acide hydrazide [III] and the later compound reaction with substituted acetophenone[IV]n to synthesized substituted acetophenone hydrazones[V-XI]. In addition synthesized4-formylpyrazole derivatives [XIIXVIII] via cyclisation substituted acetophenone hydrazones [V-XI] with Vilsmeier-Haack reagent DMF/POCl3. The compounds characterized by melting points, FTIR, 1HNMR and mass spectroscopy. The mesomorphic behavior studied by using polarized optical microscopy and
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