In this study new derivatives of Schiff bases 5-8, 1, 3-oxazepine 9-16 and tetrazoles 17-19 have been synthesized from the new starting material 1 which has synthesized the reaction of one mole of dichloro acetic acid and two moles of thiophenol, the esters 2-3 were synthesized from the reaction of compound 1 with methanol or ethanol respectively in the presence of H2SO4 as catalyst then 2, 2-dithiophenylaceto Hydrazide 4 were synthesized from the reaction of 2 or 3 with hydrazine hydrate 80%, Schiff bases 5-8 were synthesized from the reaction of 4 with appropriate aldehyde or ketone. Treatment of Schiff bases with maleic and phathalic anhydride in dry benzene to give 1, 3-oxazepen derivatives 9-16 and with sodium azide in tetrahydrofuran (THF) afforded tetrazole derivatives 17-19. All these compounds have been characterized from their melting pointes, FTIR, 1HNMR and compounds 1, 5 and 18 by mass spectrometry. Derivatives 6, 7, 11, 16, 17 and 18 were tested against inhibition of E. coli and. Staphylococcus-aureus and were all funds to be active. Scheme (1).
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 MoreThe ligand 4-amino-N-(5-methylisoxazole-3-yl)-benzene-sulfonamide(L1) (as a chelating ligand) was treated with Pd(II),Pt (IV) and Au(III) ions in alcoholic medium in order to prepare a series of new metal complexes. Mixed ligand complexes of this primary ligand were prepared in alcoholic medium in presence of the co-ligand 4,4'-dimethyl-2,2'-bipyridyl(L2) with Cu(II) ,Pd(II) and Au(III) ions. The complexes were characterized in solid state using flame atomic absorption, elemental analysis C.H.N.S, FT-IR, UV-Vis Spectroscopy, conductivity and magnetic susceptibility measurements. The nature of some complexes formed in ethanolic solution has been studied following the molar ratio method, also stability constant was studied and the complexes f
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(2)
The 4-(?-bromo acetyl)-4?-toluene sulfonanilide (2) was used as key intermediate to synthesize new heterocyclic compounds. This bromo compound was synthesized via sulfonation of amino group of p-amino acetophenone using Hinsburg method with 4-toluene sulfonyl chloride to form 4-acetyl-4?-toluene sulfonanilide (1) which is used as a starting material in this work. This compound was brominated to yield compound (2) which is used as a precursor to synthesize new five and seven membered heterocyclic compounds such as substituted 1,3-oxazoles (3,4), 1,3-thiazole derivatives (5-7), thiourea compounds (8a,b), 1,3-Thiazoline-2-thione compounds (9a-f) and 1,2,5-triazepine compounds (11a-d). The synthesized compounds were identified depending u
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Five membered heterocyclics derivatives were synthesized in this work by three routes. The first route includes the synthesis of N-benzoic acid 1,2,3,-triazole derivatives (3),(4) by diazotation of methyl-2-amino benzoate and treating the resulted salt (1) with sodium azide and ethyl acetoacetate or acetyl acetone, respectively. In the second route, derivatives of pyrazole (8) pyrazolin-5-one (9), (10) were prepared by the reaction of the salt (1) with some active methylene compounds to give the corresponding hydrazones derivatives (5-7) which then they were treated with hydrazine hydrate. The third route afforded the synthesis of three derivatives (12), (15a), (15b) of thiazolidinone by two different methods. AII compounds were confirmed b
... Show MoreA new set of metal complexes by the general formula [M(C)2(H2O)2]Cl2 has been prepared through the interaction of the new Ligand [N1, N4-bis(4-chlorophenyl)succinamide] (C) derived from succinyl chloride with 4-Chloroaniline with the transition metal ions Mn(II), Co(II), Ni(II), Hg(II), Cu(II) and Cd(II). Compounds diagnosed by TGA, 1 H, 13CNMR and Mass spectra (for (C)), Fourier-transform infrared and Electronic spectrum, Magnetic measurement, molar conduct, (%M, %C, %H, %N). These measurements indicate that (C) is associated with the metal ion in a bi-dentate fashion by nitrogen atoms (the amide group) and the octahedral composition of these complexes is suggested. The anti-bacterial action of the compounds towards three types of bacteria
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(4)
To synthesize new hydrazone derivatives of naproxen with enhanced anti-inflammatory activity and devoid the ulcerogenic side effects. Hydrazones were synthesized by conjugation of naproxen hydrazide with seven natural and synthetic aldehyde and ketone by using glacial acetic acid as catalyst. The synthesis has been carried out following simple methodology in excellent isolated yields.The structure of the synthesized derivatives has been characterized by elemental microanalysis (CHN), FTIR Spectroscopy, and other physicochemical properties.The anti- inflammatory activity of the synthesized compounds was evaluated in vivo using the egg-white induced edema model in rats, and the results of the biological assay was found to be comparable to Nap
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(15)
Pathogenic microorganisms are becoming more and more resistant to antimicrobial agents. So the synthesis of new antimicrobial agents is very important. In this work, new 5-fluoroisatin-chalcone conjugates 5(a–g) were synthesized based on previous research that showed the modifications of the isatin moiety led to the synthesis of many derivatives that have antimicrobial activity. 4-aminoacetophenone reacts with 5-fluoroisatin to form Schiff base (3), which in turn reacts with two different groups of aromatic (carbocyclic and heterocyclic) aldehydes 4(a–g) separately to form the final compounds 5(a–g). Proton-nuclear magnetic resonance (¹H-NMR) and Fourier-transform infrared (FT-IR) spectroscopy were used to confirm the chemic
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(1)
Transition metal complexes of Co(II) and Ni(II) with azo dye 3,5-dimethyl-2-(4-nitrophenylazo)-phenol derived from 4-nitoaniline and3,5-dimethylphenol were synthesized. Characterization of these compounds has been done on the basis of elemental analysis,electronic data, FT-IR,UV-Vis and 1 HNMR, as well as magnetic susceptibility and conductivity measurements. The nature of thecomplexes formed were studies following the mole ratio and continuous variation methods, Beer ' s law obeyed over a concentrationrange (1x10 -4 - 3x10 -4 M). High molar absorbtivity of the complex solutions were observed. From the analytical data, thestoichiomerty of the complexes has been found to be 1:2 (Metal:ligand). On the basis of physicochemical data tetrahedral
... Show MoreA new series polymers was synthesized from reaction starting material Bisacodyl A or [(2-Pyridinylmethylene) di-4, 1-phenylene di acetate] with hydrogen bromide, then the products were polymerized by addition polymerization from used adipoyl and glutaroyl chloride. The structure of these compounds was characterized by FT-IR, melting points, TLC, X-Ray, DSC and 1H-NMR for starting material. These compounds were also screened for their antibacterial activists?
(1)