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.
Eleven new 2,6-di-tert-butyl-4-(5-aryl-1,3,4-oxadiazol-2-yl)phenols 5a–k were synthesized by reacting aryl hydrazides with 3,5-di-tert butyl 4-hydroxybenzoic acid in the presence of phosphorus oxychloride. The resulting compounds were characterized based on their IR, 1H-NMR, 13C-NMR, and HRMS data. 2,2-Diphenyl-1-picrylhydrazide (DPPH) and ferric reducing antioxidant power (FRAP) assays were used to test the antioxidant properties of the compounds. Compounds 5f and 5j exhibited significant free-radical scavenging ability in both assays.
This work included synthesis of several new polymers of polyacryloyl chloride in two steps . The first step the included the reaction of N-( sub. or un sub. benzoyl and sub. or un sub. acetyl ) amidyl sub. 2,6- diamino -4-methyl-1,3,5-triazine (1-5) by condensation of many substituted acid chlorides with 2,6- diamino -4-methyl-1,3,5-triazine . While the second step included the reaction of polyacryloyl chloride with the produced compounds (1-5) in step (1) in the presence amount triethyl amine (Et3N) to obtain new polyimides (6-10). The prepared compounds were characterized by UV. , FT-IR, and some of them by 1H-NMR and 13C- NMR spectroscopy.
Schiff base derived from PVA and Erythroascorbic acid derivative (pentulosono-ɣ-lactone-2, 3-enedianisoate) was synthesized and characterized by Thin Layer Chromatography (TLC) and FTIR spectra, aldehyde was also characterized by (U.V-Vis), 1HNMR, 13CNMR and mass spectra. The inhibitory effect of prepared polymer on the activity of human serum Cholinesrerase has been studied in vitro. The polymer showed a remarkable activity at low concentration (4.5*10-3 – 4.5*10-8 M).
The quadrupole moment of 14B exotic nucleus has been calculated using configuration mixing shell model with limiting number of orbital's in the model space. The core- polarization effects, are included through a microscopic theory which considers a particle-hole excitations from the core and the model space orbits into the higher orbits with 6ħω excitations using M3Y interaction. The simple harmonic oscillator potential is used to generate the single particle wave functions. Large basis no-core shell model with (0+2)ћω truncation is used for 14B nucleus. The effective charges for the protons and neutrons were calculated su |
New twin compounds having four-, five-, and seven- membered heterocyclic rings were synthesized via Schiff bases (1a,b) which were obtained by the condensation of o-tolidine with two moles of 4- N,N-dimethyl benzaldehyde or 4- chloro benzaldehyde. The reaction of these Schiff bases with two moles of phenyl isothiocyanate, phenyl isocyanate or naphthyl isocyanate as in scheme(1) led to the formation of bis -1,3- diazetidin- 2- thion and bis -1,3- diazetidin -2-one derivatives (2-4 a,b). While in scheme (2) bis imidazolidin-4-one (5a,b) ,bistetrazole (6a,b) and bis thiazolidin-4-one (7a,b) derivatives were produced by reacting the mentioned Schiff bases(1a,b)with two moles of glycine, sodium azide or thioglycolic acid, respectively. The new b
... Show MoreIn this work, prepared new ligand namely 5-(2,4-dichloro-phenyl)-1,3,4-oxadiazole-2-(3H)-thion, was obtained from the 2,4-dichlorobenzoyl chloride with hydrazine, after that reaxtion with CS2/KOH in methanol.
The discovery of novel therapeutic molecules is always difficult, and there are a variety of methodologies that use the most diverse and innovative medicinal chemistry approaches. One such approach is the deuteration technique: Deuteration is the process of substituting deuterium for hydrogen in a molecule. When compared to the drug molecule, its deuterated analogues may retain the features of the original molecule and, in some cases, improve its pharmacological activity, with fewer side effects and lower toxicity. Metronidazole is a commonly used antibiotic to treat anaerobic bacterial infections, protozoal and microaerophilic bacterial infections. Met
... Show MoreThis article includes designed and synthesized for bent-shaped liquid crystal molecules starting from 5,5-diethylpyrimidine-2,4,6(1H,3H,5H)-trione and two moles of chloroacetylchloride in N, N-dimethyl formamide (DMF) and triethylamine (TEA) to product compound [I] ,then reacted the later compound with two moles of 4-hydroxybenzonitrile to yield nitrile compound [II]. Likewise, reaction 5,5-diethylpyrimidine-2,4,6(1H,3H,5H)-trione and two moles of ethylchloroacetate with fused sodium acetate in ethanol to create an ester compound [III], and then the later compound was reacted with two moles of hydrazine hydrate in ethanol to obtained hydrazide acid compound [IV]. After that, the compound [IV] reacted with two moles of ethyl acetoacetate in
... Show MoreSchiff base (methyl 6-(2- (4-hydroxyphenyl) -2- (1-phenyl ethyl ideneamino) acetamido) -3, 3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0] heptane-2-carboxylate)Co(II), Ni(II), Cu (II), Zn (II), and Hg(II)] ions were employed to make certain complexes. Metal analysis M percent, elemental chemical analysis (C.H.N.S), and other standard physico-chemical methods were used. Magnetic susceptibility, conductometric measurements, FT-IR and UV-visible Spectra were used to identified. Theoretical treatment of the generated complexes in the gas phase was performed using the (hyperchem-8.07) program for molecular mechanics and semi-empirical computations. The (PM3) approach was used to determine the heat of formation (ΔH˚f), binding energy (ΔEb), an
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