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.
Metal complexes of Mn(II), Co(II), Ni(II), Cu(II), Cd(II), Zn(II), Hg(II), Pd(II), and Pt(II) with Schiff base ligand (LH) derived from 2,5-dichloroaniline and 2-hydroxy-5-metheylbenzalaldehyde were synthesized and characterized using a variety of spectrophotometric techniques The findings of the spectroscopic analysis indicated that (LH) behaved as a binary coordinating agent to the metal ion by the N and O atoms, and the geometry shape of the complexes was octahedral, with the exception of the Pd and Pt complexes, which had a square planar geometry. Using the DPPH radical scavenging method, we investigated the antimicrobial activity of the compound against Staphylococcus aureus and Escherichia coli, as well as the antifungal activity of t
... Show MoreThe mixed ligand complexes of Schiff base ligand (Z)-2-(((4-bromo-2-methylphenyl) imino) methyl)-4-methylphenol (L) with some metals ion (II); Mn(1), Co(2), Ni(3), Cu(4), Zn(5) Cd(6) and Hg(7) and 1,10-Phenanthroline (phen) were Synthesis and characterized by the mass and 1HNMR spectrometry (ligand Schiff base), the FTIR, UV-visible and the flame atomic absorption (A.A) spectrum, the C.H.N analysis and the chlorine content, in addition to measuring the magnetic sensitivity of the complexes. All the complexes had octahedral geometry. The bioactivity activity for compounds against; Rhizopodium, Staphylococcus aureus and Escherichia coli, the compounds showed different efficacy towards these microorganisms
Due to its association with hepatocellular carcinoma and being one of the ten most common malignancies worldwide, hepatitis C viral infection has become a severe public health concern. Therefore, establishing an accurate, reliable and sensitive diagnostic test for this infection is strongly advised. Real-time polymerase chain reaction (PCR) has been created to achieve this purpose. The current study was established to investigate the hepatitis C virus among Iraqi patients with chronic renal failure and to detect the virus immunologically by the fourth generation enzyme-linked immunosorbent assay technique and molecularly by real-time PCR. As a result, out of 50 patients with chronic renal failure undergoing dialysis, 39 patients tes
... Show MoreThe aim of this work was to develop and validate a rapid and low cost method for estimation of ibuprofen in pharmaceutical suspensions using Reverse-Phase High Performance Liquid Chromatography. The proposed method was conducted and validated according to International Conference on Harmonization (ICH) requirements. The chromatographic parameters were as follows: column of octyldecylsilyl C18 with dimensions (150 × 4.6) mm, mobile phase composed of acetonitrile with phosphoric acid with a ratio of 50 to 50 each using isocratic mode, flow rate of 1.5 mL/min and injection volume of 5 μL. The detection was carried out using UV detector at 220 nm. The method was validated and showed short retention time for ibuprofen peak at 7.651 min, wit
... Show MoreThe objective of this study is to determine levels of some pro-inflammatory cytokines (IL-12 and SIL-2R) in pregnant women with polycystic ovary syndrome (PCOS) and also to determine incidence of spontaneous abortion during first trimester in pregnant women with PCOS compared with non-PCOS pregnant women. This Study was performed on (93) women, consisted of: 1- (63) pregnant women during the first trimester, which included:A- (33)PCOS pregnant women and subdivided into the following groups: (20) successful pregnant PCOS, (7) blighted Ovum PCOS and (6) missed abortion PCOS. B- (30) non-PCOS pregnant women, which included: (27) successful pregnant control and (3) non-PCOS pregnant women were withdrawn from this study because of their abortion
... Show MoreNaproxen is non-steroidal anti-inflammatory drug, which has antipyretic and anti-inflammatory effect. It is extensively bound to plasma albumin, and exhibits gastric toxicity, so it may be more efficient to deliver the drug in its sustained release dosage form and adequate blood level is achieved. Three liquid formulations with in situ gelling properties have been assessed for their potential for the oral sustained delivery of naproxen . The formulations were dilute solutions of: (a) pectin; (b) gellan gum and; (c) sodium alginate, all containing complexed calcium ion that form gels when these ions are released in the acidic environment of the stomach . The viscosity of the sols and drug release were measured, and was found to be depende
... Show MoreThis work involves synthesis and characterization of some new 1, 3, 4-thiadiazole or pyrazoline derivatives heterocyclic containing indole ring. The new 2-amino-1, 3, 4-thiadiazole derivatives [IV] and [V] a, b were synthesized by cyclization reaction of 2-methyl-1H-indole-carbothiosemicarbazide [III] in H2SO4 acid or by reaction of indole-3-acetic acid or indole-3-butanoic acid with thiosemicarbazide in the presence of phosphorous oxychloride, respectively. Amide derivatives [VI]-[VIII] were synthesized by the reaction equimolar of 2-amino-1, 3, 4-thiadiazoles and (acetyl chloride, benzoyl chloride, anisoyl chloride and heptanoyl chloride) in DMF and pyridine as accepter. The new pyrazolone derivatives [XI] a, b were synthesized from heati
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