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.
BACKGROUND: Acute coronary syndrome (ACS) is the clinical manifestation of acutely diminished coronary arterial blood supply. The rate of increase of intraventricular pressure during isovolumetric contraction (left ventricular dP/dt) represents the rate of change of pressure during ejection. OBJECTIVE: The aim of this study is to evaluate the usefulness of the rate of increase of intraventricular pressure during isovolumetric contraction (dP/dt) in assessment of left ventricular function in patients with acute coronary syndrome and its relation to certain clinical and echocardiographic features. PATIENTS AND METHODS: The study is a cross sectional study including 50 patients with an established diagnosis of acute coronary syndrome. The
... Show MoreDengke Naniura is a traditional food from Sumatera Utara, Indonesia, that is produced through fermenting process, and this food is believed to contain high probiotics. The objective of the current research is to determine the potential of LAB as a probiotic that has been obtained from Dengke Naniura. Dengke Naniura was traditionally prepared from Cyprinus carpio. Four LABs have been successfully isolated from Dengke Naniura, such as D7DA3, D7B3, D7DBF and D7DN3. Those four LAB isolates were identified as Lactobacillus sp. This result has been confirmed by the non-spore forming bacterium, non-motile, and Gram-positive. Also, it has been supported by biochemical test, for the example Voges Proskauer, catalase test, Methyl
... Show MoreThe manganese doped zinc sulfide nanoparticles were synthesized by simple aqueous chemical reaction of manganese chloride, zinc acetate and thioacitamide in aqueous solution. Thioglycolic acid is used as capping agent for controlling the nanoparticle size. The main advantage of the ZnS:Mn nanoparticles of diameter ~ 2.73 nm is that the sample is prepared by using non-toxic precursors in a cost effective and eco-friendly way. The structural, morphological and chemical composition of the nanoparticles have been investigated by X-ray diffraction (XRD), Scanning Electron Microscopy (SEM) with energy dispersion spectroscopy (EDS) and Fourier transform infrared (FTIR) spectroscopy. The nanosize of the prepared nanoparticles was elucidated by Scan
... Show MoreThis study investigates the characterization and mechanical performance of Stone Mastic Asphalt (SMA) mixtures modified with two types of polymers: styrene–butadiene–styrene (SBS) and high-molecular-weight polyethylene (PE). Neat asphalt cement PG 64-16 was modified using a higher content of SBS and PE at concentrations of 6%, 7%, and 8% by weight of asphalt through the dry blending method to produce Highly Modified Asphalts (HiMA). The physical and rheological properties of the modified binders were evaluated using penetration, softening point, rotational viscosity, and dynamic shear rheometer (DSR) tests. Also, their phase compatibility and morphological changes were evaluated using the storage stability testing and scanning electron
... Show MoreDespite the antiplaque effect of mouth-rinsing with a combination composed of miswak (Salvadora persica L.) and green tea (Camellia sinensis var. assamica) extracts, no data are available regarding its effect on gingival tissue at the molecular level. This pilot study aimed to assess the effect of oral rinsing with this combination on gingival crevicular fluid (GCF) flow and IL-1β levels. Ten subjects rinsed with either the combination, 0.12% chlorhexidine gluconate (CHX) or distilled water without toothbrushing for 4 days after receiving baseline polishing. GCF IL-1β concentration, influx, resting volume and plaque quantity were measured at baseline and after 4 days for each intervention. No significant differences in GCF flow or
... Show MoreObjective: Carbamazepine is typically used for the treatment of seizure disorders and neuropathic pain. One of the major problems with this drug is its low solubility in water; therefore the objective of this study was to enhance the solubility of carbamazepine by complexation with cyclodextrin to be formulated as effervescent and dispersible granules.Methods: Solvent evaporation method was used to prepare, binary (Carbamazepine/β-cyclodextrin) complex and ternary (Carbamazepine/β-cyclodextrin/hydroxypropyl methyl cellulose (HPMC E5). The more soluble complex will be further formulated as unit dose effervescent and dispersible granules. The complexes were evaluated for their solubility, drug content, percentage practical yield and
... Show MoreThe aim of present study was to develop solid and liquid self-microemulsifying drug delivery system of poorly water soluble drug mebendazole using Aerosil 200 as solid carrier. Microemulsions are clear, stable, isotropic liquid mixtures of oil, water and surfactant, frequently in combination with a co-surfactant having droplet size range usually in the range of 20-250 nm. Oleic acid, tween 80 and polypropylene glycol were selected as oil, surfactant and co-surfactant respectively and for preparation of stable SMEDDS, micro emulsion region was identified by constructing pseudo ternary phase diagram containing different proportion of surfactant: co-surfactant (1:1, 2:1 and 3:1), oil and water. In brief S/ CoS mix means su
... Show MoreBackground: Acute myeloid leukemia (AML) is a genetically heterogeneous leukemia characterized by abnormal myeloid blast accumulation, disrupting normal hematopoiesis and leading to rapid progression. Objective: To investigate SNPs within the 3’UTR of the CCAAT/enhancer-binding protein alpha (CEBPA) gene and its association with AML in Iraqi patients. Methods: The study was carried out on 120 AML patients classified into newly diagnosed, induction chemotherapy, and consolidation chemotherapy stages (40 each), and 40 individuals as a control group. Genomic DNA was extracted from AML patients and controls, followed by PCR amplification and Sanger sequencing of the 3’UTR region of the CEBPA gene. The AML patients were characterized
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