New hydrazone derivatives of Fenoprofen were synthesized and evaluated for their anti-inflammatory activity by means of egg white induced paw edema method. All the synthesized target compounds were characterized by FT-IR spectroscopy, 1HNMR analysis and by measure of their physical properties. The synthesis of the target compounds(H1-H4) was accomplished by multistep reaction procedures. The synthesized target compounds were show activity in reducing paw edema thickness and their anti-inflammatory effect was comparable to that of the standard (Fenoprofen) except for compound H3 which show anti-inflammatory activity higher than Fenoprofen.
Objective: Synthesized a series of new thiourea (TU) derivatives, tested their antioxidant activity, and investigated their expected biological activity by theoretical study (computational methods). Methods: The derivatives were made using a one-pot reaction with two steps. Initially, succinyl chloride was mixed with KSCN to make succinyl isothiocyanate. Then, primary and secondary amines were used to make TU derivatives. The theoretical studies were done by Swiss ADME and molecular docking via Genetic Optimization of Linkage Docking (GOLD). Then evaluate antioxidant activity using the DPPH scavenging method. Results: FT-IR, 1H NMR, and 13C NMR spectroscopy show the verification of all the prepared derivatives. Compounds (II), (VIII),
... Show MoreThe new C-5 schiff bases derived from D-erythroascorbic acid contaning pyrimidine unit were synthesized by condensation of D-erythroascorbic acid with aromatic amine (containing pyrimidine unit)in dry benzene using glacial acetic acid as a catalyst. D-erythroascorbic acid was synthesized by four steps(Schem 1), while the aromatic amine which is containing oxopyrimidine or thiopyrimidine synthesized by the reaction of chalcone urea or thiourea in acid or basic medium, respectively . The structure of synthesized compounds have been characterized by their melting
... Show MoreSeveral new derivatives of 1, 2, 4-triazoles linked to phthalimide moiety were synthesized through following multisteps. The first step involved preparation of 2, 2-diphthalimidyl ethanoic acid [2] via reaction of two moles of phthalimide with dichloroacetic acid. Treatment of the resulted imide with ethanol in the second step afforded 2,2-diphthalimidyl ester[3] which inturn was introduced in reaction with hydrazine hydrate in the third step ,producing the corresponding hydrazide derivative[4] .The synthesized hydazide was introduced in different synthetic paths including treatment with carbon disulfide in alkaline solution then with hydrazine hydrate to afford the new 1,2,4-triazole[10] .Reaction of com
... Show MoreNew 2-amino thiazole ,oxodiazole, sulphonilamide and diazin derivatives of N-(α-chloro aceto)-3-(tolyl imino)-5-bromo-2-oxo-indole(2) have been synthesized .The preparation process started by the reaction of 5-bromo isatin with P-toluidine in the presence of glacial acetic acid and dimethylformamide(DMF) as a solvent to give 3-(tolyl imino)5-bromo-1H-indole-2-one.(1), Compound (1) with sodium hydride in dimethylformamide(DMF) at 0C0 gave a suspension of the sodium salt of Schiff base derivative and subsequent reaction with monochloroacetylchloride obtained the intermediate compound(2).Compound(2) was reacted with different reagents in four routes.The first route involved direct reaction with substituted 2-aminobenzothiazole u
... Show MoreSeveral new derivatives of 1, 2, 4-triazoles linked to phthalimide moiety were synthesized through following multisteps. The first step involved preparation of 2, 2-diphthalimidyl ethanoic acid [2] via reaction of two moles of phthalimide with dichloroacetic acid. Treatment of the resulted imide with ethanol in the second step afforded 2, 2-diphthalimidyl ester [3] which inturn was introduced in reaction with hydrazine hydrate in the third step, producing the corresponding hydrazide derivative [4]. The synthesized hydazide was introduced in different synthetic paths including treatment with carbon disulfide in alkaline solution then with hydrazine hydrate to afford the new 1, 2, 4-triazole [10]. Reaction of compound [10] with different alde
... Show MoreHeterogeneous organic compounds play an important role in our daily life as they contribute in many medical and industrial fields and are in continuous development as a result of the preparation of new derivatives with different properties. From this premise, the goal of this work appears, which is preparation of (four, five, six, and seven) membered ring systems derived from furfural, by its reaction with different aromatic aldehydes, and record their antioxidant activity by using free radical scavenging method of DPPH radicals. The new ring systems are synthesized by reacting the prepared Schiff-bases with different ring closure agents (chloroacetyl chloride, mercaptoaceticacid, anthranilic acid, and phthalic anhydride), the prep
... Show MoreBackground: Systemic sclerosis (SSc) is a chronic autoimmune illness, which is consider by three main features: Sclerotic changes in the skin and internal organs, Vasculopathy of small blood vessels, Particular autoantibodies (1). The most important autoantibodies appeared significantly in SSc patients are anti-topoisomerase I autoantibody (Scl-70), anti-centromere autoantibody (ACA), and anti-RNA polymerase III autoantibody (RNAP3) (2). Anti-centromere antibodies (ACA) are infrequent in rheumatic conditions and in healthy persons but occur commonly in limited systemic sclerosis (CREST syndrome), and rarely appeared in the diffuse form of systemic sclerosis (3). Anti-Ro/SSA and antiLa/SSB, antibodies directed against Ro/La ribonucleoprot
... Show MoreA series of new Bis-1,4-Butane -1,3,4 – Oxadizole derivatives [III a-j] were synthesized from adipic acid dihydrazide and different aromatic acids in the presence of phosphours oxychloide. There compounds were characterized by their IR, microanalysis, and mass spectral data. In vitro antimicrobial were synthesized. In vitro antimicrobial activity of these compounds against (Gram negative) and (Gram positive) were reported, some of these compounds prepared derivatives exhibited antimicrobial activity
Objective:This study involved synthesis of a new series of different five-membered heterocyclic derivatives, testing their antioxidant activity, and examining their potential in vitro antimicrobial agents. Methods: The synthesis of the derivatives involved a three-step process. Initially, succinyl chloride was reacted with methanol, followed by a reaction with 80% hydrazine hydrate through a nucleophilic addition-elimination mechanism, resulting in the formation of succinohydrazide (I). This compound was then employed as a precursor for the synthesis of Schiff bases (II), and (III) by reacting it with m-nitro benzaldehyde and p-nitro benzaldehyde. Following this, a ring closure reaction was applied using thioglycolic acid, glycolic acid,
... Show MoreInthis study new derivatives of Schiff bases and nucleoside analogues have been synthesized from the starting material D-glucose after a series of reactions. Derivative 1 was prepared from D-glucose then react with P-bromoacetophenone gave derivative 2 was reacted with dimethyl sulfoxide and acetic anhydride for dehydration a molecule of water gave 3. The spiro ring was prepared at 3-position from the reaction of 3 derivative with 1-phenyl-2–thioureagave 4. The protection group at 1 position was removed by using acetic acid fllowed by periodate oxidation to obtain 6. Reaction of 6 with hydrazide derivative at once and dtriazole derivative at another gave 8 and 9 respectively. Compound 6 was reduced to gave derivative 7. The 1-hydroxylgrou
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