Mefenamic acid (MA) is one of the non-steroidal anti-inflammatory drugs, it is widely used probably due to having both anti-inflammatory and analgesic activity, the main side effects of mefenamic acid include gastrointestinal tract (GIT) disturbance mainly diarrhea, peptic ulceration, and gastric bleeding. The analgesic effects of NSAIDs are probably linked to COX-2 inhibition, while COX-1 inhibition is the major cause of this classic adverse effects. Introduction of thiazolidinone may lead to the increase in the bulkiness leads to the preferential inhibition of COX-2 rather than COX-1 enzyme. The study aimed to synthesize derivatives of mefenamic acid with more potency and to decrease the drug's potential side effects, new series of 4-thiazolidinone derivatives of mefenamic acid were synthesized IVa-g. The synthetic procedures for target compounds and their intermediates are designed to be as follows: acylation of secondary amine of mefenamic acid by chloroacetylchloride to produce compound (I), then reaction between compound (I) and hydrazine hydrate to form hydrazine derivative of mefenamic acid (compound II). After that, Schiff base formation by addition of seven benzaldehyde derivatives and finally, cyclization in presence of thioglycolic acid to form 4-thiazolidinone heterocyclic ring. The characterization of the titled compounds has been established on the basis of their spectral FTIR, 1HNMR data, and by measurements of their physical properties. In vivo acute anti-inflammatory effect of the synthesized compounds was evaluated in rats using egg-white induced edema model of inflammation. The tested compounds and the reference drug produced significant reduction of paw edema with respect to the effect of dimethyl sulfoxide 10%v/v (control group). Compound IVe showed more potent effect than mefenamic acid at 240-300 min, while at time 300 min, compounds IVa and IVd exhibit more potent anti-inflammatory effect than mefenamic acid (50mg/kg, i.p.) as they reduced paw edema significantly more than mefenamic acid at mentioned intervals (p<0.05) . On the other hand compound IVc exhibited lower anti-inflammatory effect.
1, 3, 4-oxadiazole-5-thion ring (2) successfully formed at position six of 2-methylphenol and five of their thioalkyl (3a-e). Furthermore 6-(5-(Aryl)-1, 3, 4-oxadiazol-2-yl)-2-methylphenol (5a-i) were formed at position six by two method. The first method was from cyclization their correspondinghydrazones (4a-e) of 2-hydroxy-3-methylbenzohydrazide (1) using bromine in glacial acetic acid. The second method was from cyclization the hydrazide with aryl carboxylic acid in the presence of phosphorusoxy chloride. The newly synthesized compounds were characterized from their IR, NMR and mass spectra. The antioxidant properties of these compounds were screened by 2, 2-Diphenyl-1-picrylhydrazide (DPPH) and ferric reducing antioxidant power (FRAP) a
... Show Morethe physical paraneters of oxadizole derivaties as donor molecules have been measured the charge transfer and methanol as solvent have been estimated from the electonic spectra
MR Younus, Al-A'DAB, 2011
The present study was conducted to examine toxicological effects of copper sulfate (Cu) in common carp fish (Cyprinus carpio L.). The LC50 (median lethal concentrations) of copper on Cyprinus carpio were 3.64, 3.36, 3.04, 2.65 mg/L respectively. In general, behavioral responses of the fishes exposed to copper included uncontrolled swimming, erratic movements, loss of balance, swam near the water surface with sudden jerky movements. Haematological parameters such, red blood cells (RBC), white blood cells (WBC), haemoglobin (Hb), Packed cell volume (PCV), mean cell volume (MCV) mean cell haemoglobin (MCH), and mean corpuscular hemoglobin concentration (MCHC) were studied. The obtained results indicated that the (RBC) and (WBC) have increas
... Show MoreThe preliminary test of the compounds N [2– (3,4–dimethoxy nitrobenzene oxazepine– 2,3–dihydro–4,7–dione]–5–mercupto–2–amino–1,3,4–thiadiazol [A] and N [ 2–anthralidene– 5– ( 2–nitrophenyl ) –1,3–oxazepine–4,7–dione–2–d](5–mercapto–1,3,4–thiadiazole–2–amin) [B] , showed that they possess high activity against some positive and negative bacteria , like pseudomonas aeruginosa (pseudo.), Escherichia coli (E-coli), staphylococcus aureus (sta.) and Bacillus subtilis (Ba.) and finally there is a study of the effect of some antibiotics like streptomycin (S), gentamycin (GN), chloramphenicol (C) and Nalitixic acid (NA) in order to compare the differences in effects. In the present study, results
... Show MoreDespite extensive investigations, an effective treatment for sepsis remains elusive and a better understanding of the inflammatory response to infection is required to identify potential new targets for therapy. In this study we have used RNAi technology to show, for the first time, that the inducible lysophosphatidylcholine acyltransferase 2 (LPCAT2) plays a key role in macrophage inflammatory gene expression in response to stimulation with bacterial ligands. Using siRNA- or shRNA-mediated knockdown, we demonstrate that, in contrast to the constitutive LPCAT1, LPCAT2 is required for macrophage cytokine gene expression and release in response to TLR4 and TLR2 ligand stimulation but not for TLR-independent stimuli. In addition, cells transfe
... Show MoreObjective(s): To measure serum C-reactive protein (CRP) titer as a predictive diagnosis of acute hepatitis C virus (HCV)
infection.
Methodology: Two hundred and ten patients with acute HCV infection and 234 apparently healthy individuals as
control group were enrolled in this study in Baghdad medical city (Teaching Laboratories). The patents include
74(35.2%) females and 136 (64.8%) males with mean age (27±16.5) years. The control group includes 114 (48.7%)
females and 120 (51.3%) males with mean age (26±5.8) years. Blood samples were collected from out patients from
Alfadul in Baghdad city. Sera were separated and stored at 20 0
C. The diagnosis of acute HCV infection was based on
detection of HC Ag and anti- H
Background : It has been suggested that pretreatment with a statin agent prior to
myocardial infarction limits myocardial
creatine kinase release, and thus may act to
limit myocardial infarct size in humans.
Objective : To examine the effect of very
early statin initiation for acute myocardial
infarction (AMI), to the extent of
myonecrosis as manifested by peak serum
creatine kinase levels.
Methods : Patients with AMI admitted to AlKindy teaching hospital cardiac care unit
from 1st February 2007 to 28th February
2008, who fulfilled the inclusion criteria
cited in the present study, were randomly
assigned into two study groups. The statin
group patients have received a single oral
dose of 40 mg
The present study aimed to investigate the acetamiprid effects on biochemical aspects in albino mice. Thirty albino mice at the age of 6-8 weeks and average weight 25±5 g were divided into three groups each having ten (10) healthy mice. The first group was orally administrated with distilled water while the second and third groups were orally administrated with 50 mg/mL and 100 mg/mL respectively of acetamprid (0.1 mL) daily for one week. LD50 of acetamiprid was measured and found to be 200 mg/kg. The parameters of evaluations included liver function using Aspartate Aminotransferase (AST), Alanine Aminotransferase (ALT) and Alkaline Phosphatase (ALP). Lipid profile was anal
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