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.
In this work, the precursor [2-(1,5-dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazol-4-ylimino)acetic acid] was synthesised from 4-aminoantipyrine and glyoxylic acid, this precursor has been used in the synthesis of new multidentate ligand [2-((E)-3-(2-hydroxyphenylimino)-1,5-dimethyl-2-phenyl-2,3-dihydro-1H-pyrazol-4-ylimino)acetic acid][H2L] type (N2O2). The ligand was refluxed in ethanol with metal ions [VO(II), Mn(II), Co(II) and Ni(II)] salts to give complexes of general molecular formula:[M(H2L)2(X)(Y)].B, where: M=VO(II), X=0, Y=OSO3-2, B=2H2O; M=Mn(II),Co(II) ,X=Cl, Y=Cl, B=0; M=Ni(II), X=H2O, Y=Cl, B=Cl. These complexes were characterised by atomic absorpition(A.A), F.T-I.R., (U.V-Vis)spectroscopies (1H,13C NMR for ligand only), alon
... Show MoreIn this work, the preparation of some new oxazolidine and thiazolidine derivatives has been conducted. This was done over two steps; the first step included the synthesis of Schiff bases A1-A5 in 72-88% yields by the condensation of isonicotinic acid hydrazide and aldehydes. The second step includes the cyclization of derivatives A1-A5 with glycolic acid and thioglycolic acid to obtain the desired products, oxazolidine derivatives B1-B5 (44-60% yields) and thiazolidine derivatives C1-C5 (41-61% yields), respectively. The structure of the prepared compounds was characterized using FT-IR, 1H NMR, and 13C NMR spectroscopy. Some of the produced compounds were tested for antioxidant properties.
Certain cyclic amine derivatives of metronidazole via acetate spacer were prepared. Cyclic amines used are piperidine and piperazine to improve the physicochemical properties and reduce some of metronidazole side effects. This is believed to be done by modification of its structural features to get prodrugs with improved properties over that of metronidazole. The present work includes esterification of metronidazole with choroacetic acid, N-alkylation of the cyclic amines by the halogenated ester and characterization of their structures by spectral(UV and IR) and elemental(CHN)analysis.The melting points, degree of solubilities and partition coefficients were also determined. Both metronid
... Show MoreNew heterocyclic compounds derived from 2-Morpholino-1,8-naphthyridine-4-carboxylic acid such as oxadiazolo, thiadiazolo – thione and triazolo-thione have been prepared and characterized on the basis of IR and 1H NMR spectra data. The hydrizide compound was utilized as a starting material for preparing of these compounds. The second part of this study involves the biological studies of some of these naphthyridine derivatives by using three different kinds of bacteria namely: Staphylococcus aureus, Pseudomonas aeruglnosa and Escherichia coli. The data indicated that some of these compounds have a good activity against the tested bacteria in comparison to antibiotics.
Isatin (1H-indole-2, 3-dione) and its analogs are an important class of heterocyclic compounds. N-benzyl isatins and Schiff bases of isatin analogs have been reported to demonstrate a variety of biological activities. This work illustrates the synthesis of new N-benzylisatin Schiff bases and studies their biological activity. Firstly, Isatin and its analogs; 5-methoxyisatin, 5-fluoroisatin reacted with benzyl iodide to obtain N-benzylated derivatives of isatins 2 (ac). Secondly, these compounds were reacted with different amines (sulphanilamide and 4-methyl sulphonyl aniline) separately, to obtain Schiff bases compounds 3 (ac) and 4 (ac), respectively. The synthesized compounds were characterized by using FT-IR and 1HNMR spectroscopy. The s
... Show MoreD-mannose sugar was used to prepare [benzoic acid 6-formyl-2, 2-dimethyl-tetrahydrofuro [3, 4-d][1, 3] dioxol-4-yl ester](compound A). The condensation reaction of folic acid with (compound A) resulted in the formation of new ligand [L]. These compounds were characterized by elemental analysis CHN, atomic absorption AA,(FT-IR),(UV-Vis), TLC, ES mass (for electrospray), molar conductance, and melting point. The new tetradentate ligand [L], reacted with two moles of some selected metal ions and two moles of (2-aminophenol),(metal: ligand: 2-aminophenol) at reflux in water medium to give a series of new complexes of the general formula K2 [M2 (L)(HA) 2] where M= Co (II), Ni (II), Cu (II) and Cd (II). These complexes were characterized by eleme
... Show MoreD-mannose sugar was used to prepare [benzoic acid 6-formyl-2,2-dimethyl-tetrahydrofuro[3,4-d][1,3]dioxol-4-yl ester] (compound A). The condensation reaction of folic acid with (compound A) resulted in the formation of new ligand [L]. These compounds were characterized by elemental analysis CHN, atomic absorption A.A, (FT-I.R.), (U.V.-Vis), TLC, E.S. mass (for electrospray), molar conductance, and melting point. The new tetradentate ligand [L], reacted with two moles of some selected metal ions and two moles of (2-aminophenol), (metal : ligand : 2-aminophenol) at reflux in water medium to give a series of new complexes of the general formula K2[M2(L)(HA)2] where M= Co(II), Ni(II), Cu(II) and Cd(II). These complexes were characterized by elem
... Show MoreIn this study the new azo compounds (3compounds) for nitrogen bases (Adenine and Cytosine) are synthesized through two reaction steps (formation of diazonium salt and coupling reaction). The compounds have been characterized by FTIR, melting point, and ultra-violate (UV) spectra. All synthesized compounds have been estimated in vitro for their antimicrobial activities against two species of bacteria(E.coli, S.aureus)and one kind of fungi ( Aspergillus flavus) .The results show that these compounds have very good antibacterial and antifungal activities especially compounds 1 and 3.To study the effect of these compounds were making some physiological tests on rats are made ,the results of hematological study showed decreasing level of
... Show MoreNewly prepared derivatives of Heterocyclic of dicarboxylic acid include 1, 2, 4-Triazoledicarboxylic acid. Thiocarbohydrazine (TCH) reacts with aliphatic and aromatic dicarboxylic acids, and when these resulting compounds interact with compounds containing a group of carbonyl they result in Schiff base, which are very important in the industrial and medical fields and the acids used (oxalic acid, succinic, terephthalic) to prepare the triazole, then the reaction with Para-chlorobenzendihaide. and some physical properties were measured for these products. The biological activity of the prepared compounds has been studied, and it has been shown that they have different effects on the bacteria, compounds prepared with Fourier Transform Infrare
... Show MoreNewly series of 6,6’-((2-(Aryl)dihydropyrimidine-1,3(2H,4H)-diyl)bis(methylene))bis(2-methoxy phenol) (3a-i) were synthesized from cyclization of 6,6’-((propane-1,3-diylbis (azanediyl)) bis(methylene)) bis(2-methoxyphenol) with several aryl aldehyde in the presence of acetic acid. The newly compounds characterized from their IR, NMR and EIMs spectra. The antioxidant capacity of these compounds screened by utilizing DPPH and FRAP assays. Compounds 3g and 3i exhibited significant antioxidant capability in both assays. Docking study for these compounds as a potential inhibitors of gyrase enzyme were carried out. Compound 3g exhibited significant inhibition with binding free energies (DG) higher than novobiocin. compounds 2, 3a, 3b, 3
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