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.
A new compounds of 2,4-substituted-1,3- thiazole containing amines [I] and [II], Schiff bases [IV] and [V], amides [VI]-[X],esters [XI] - [XIII], thiazolidinones [XIV]-[XVIII] and 1,3-oxazepines [XIX]-[XXV] were Synthesized and characterized by melting points, FTIR spectroscopy, elemental analysis, 1HNMR,13CNMR, dept135and Mass spectroscopy. The liquid crystalline properties of the synthesized compounds were verified by using hot-stage polarizing optical microscopy (POM) and differential scanning calorimeter (DSC). The compound [I] was found to be nematic textures (N). The first series of this study [II]n display only enantiotropic nematic phase when n=1-5 while the compounds with n =6-8 display two mesophasese smectic C(SmC) and nematic ph
... Show MoreThe new 4-[(7-chloro-2,1,3-benzoxadiazole)azo]-4,5-diphenyl imidazole (L) have been synthesized and characterized by micro elemental and thermal analyses as well as 1H.NMR, FT-IR, and UV-Vis spectroscopic techniques. (L) acts as a ligand coordinating with some metal ionsV(IV), Fe(III), Co(II), Ni(II), Cu(II), and Zn(II). Structures of the new compounds were characterized by elemental and thermal analyses as well as FT-IR and UV-Vis Spectra. The magnetic properties and electrical conductivities of metal complexes were also determined. Study of the nature of the complexes formed in ethanol following the mole ratio method.. The work also include a theoretical treatment of the formed complexes in the gas phase, this was done using the (hyperch
... Show MoreThis paper concerned with development of a spectrophotometric method for the determination of paracetamol, based on the diazotisation and coupling reaction with anthranilic acid in basic medium, to form an intense yellow coloured, water-soluble and stable azo-dye which shows a maximum absorption at 421nm. Beer’s law is obeyed over the concentration range of 1.0-10 µg/ml; with molar absorptivity of 2.1772×104 L.mol -1.cm-1 and Sandell’s sensitivity index 6.9446 µg.cm-2. The method has been applied successfully for the determination of paracetamol in pharmaceutical formulation.
This study aimed to statement jet stream and its impact in the anti-cyclone affecting the climate of Iraq. Through the use of simple correlation coefficient ( Pearson ) that there is a very strong relationship between high- Siberian and both of the jet stream especially during the winter or over the stations of North . Therefore we, observe the relationship be significant in most of the winter months , spring and autumn . Statistically significant , but are different between station and another station , while the study come to another Anti-ciyclon have a real ,significant and statistically relationship corrclation . But this relationship is less than which found in are much less it with the Siberian high , it depends on the type of stat
... Show MoreA potentiostatic study of the behaviour of Inconel (600) in molar sulphuric acid has been carried out over the temperature range 293-313 K. Values have been established for the potentials and current densities of the corrosion, active-passive transition, passivity and transpassive states. For corrosion, the current density (ic) and potential (Ec) have been determined from well-defined Tafel lines. The potential and current density prior to the commencement of passivity have been obtained corresponding respectively to the critical potential (Ecr( and to the current density (icr) for the active-passive transition state. The passive range was defined by the respective potentials and current densities for passive film formation and dissolutio
... Show MoreFumonisin B1 is toxic secondary metabolites compound produced by Fusarium spp. on maize and maize products causes health problems to human and animal. Therefore, this research is planned to study the effect of FB1 on the expression of TLR-2 & 4 in liver and kidney cells of mice. Four group of male mice were orally administrated with single dose of FB1 toxin as the following: 0 ppb, 800 ppb, 1200 ppb and 1600 ppb. After two weeks all animals were sacrificed, liver and kidney autopsies were taken and the level of TLR-2 & 4 detected in each four group by immunohistochemistry technique (IHC). According to the IHC examination of groups (1, 2, 3 and 4) strong expression of TLR2 in liver and kidney were (0%, 33.3%, 100%, 100%), respectively. This
... Show MoreNew ligand of N-(pyrimidin-2-yl carbamothioyl)acetamide was synthesized and its complexes with (VO(II), Mn (II), Cu (II), Zn (II), Cd (II) and Hg (II) are formed with confirmation of their structures on the bases of spectroscopic analyses. Antimicrobial activity of new complexes are studied against Gram positive S. aureus and Gram negative E. coli, Proteus, Pseudomonas. The octahedral geometrical structures are proved depending on the outcomes from the preceding procedures. Keywords: pyrimidin-2-amine, acetyl isothiocyanate, complexes, Antimicrobial activity