A new series of schiff base and aminothiadiazole derivatives of N- substituted phthalimide (I-VI) were synthesized. In this work, the intermediate 4-(1,3-dioxoisoindolin-2-yl)benzaldehyde compound (I), was formed by reaction of 4-amino benzaldehyde with phthalic anhydride in glacial acetic acid(GAA). A series of Schiff bases (IV-VI) was prepared by the reaction of benzidine with compound (I) in ethanol and presence of GAA as a catalyst to form compound (IV) which react with compound (I) and p-nitro benzyldehyde to give compound (V) and (VI) respectively. A new phthalimide thiosemi-carbazone derivative (ll) was prepared by reaction of compound (l) with thiosemi-carbazide HCl in the presence of equimolar amount of sodium acetate. Finally, a new phthalimide containing (1,3,4- thiadiazole ring) compound (III) was formed by bromine mediated “oxidative intramolecular cyclization” of compound (I) in the presence of sodium acetate. All of the final target compounds' structures were successfully synthesized and confirmed using analytical and spectroscopic data. These compounds were identified and confirmed by melting points, TLC, FT IR, and 1H NMR. While the antimicrobial effect of the new derivatives has been assessed in vitro against G-positive, G-negative bacteria and fungi activity. All screened compounds exhibited no activity against G-positive bacteria (Staph. Aureus, and Bacillus subtilis). Many of synthesized compounds displayed moderate effect against “G-negative bacteria Escherichia coli, and Klebsiella pneumonia and against Candida tropicalis”. While the best antifungal activity was obtained from compound I which has high activity against Candida tropicalis.
A new ligand [N-(4-nitrobenzoylamino)-thioxomethyl] phenylalanine is synthesized by reaction of 4-nitrobenzoyl isothiocyanate with phenylalanine (1:1). It is characterized by micro elemental analysis (C.H.N.S.), FT-IR, (UV-Vis) and 1H and 13CNMR spectra. Some metals ions complexes of this ligand were prepared and characterized by FT-IR, UV-Visible spectra, conductivity measurements, magnetic susceptibility and atomic absorption. From results obtained, the following formula [M(NBA)2] where M2+ = Mn, Co, Ni, Cu, Zn, Pd, Cd and Hg, the proposed molecular structure for these complexes as tetrahedral geometry, except copper and palladium complexes are have square planer geometry.
In this paper, some series of new complexes of Mn(II), Co(II), Ni (II) Cu(II) and Hg(II) are prepared from the Schiff bases (L1,L2). (L1) derived from 4-aminoantipyrine and O-phenylene dia mine then (L2) derived from (L1) and 2-benzoyl benzoic acid. Structural features are obtained from their elemental microanalyses, molar conductance, IR, UV–Vis, 1H, 13CNMR spectra and magnetic susceptibility. The magnetic susceptibility and UV–Vis, IR spectral data of the ligand (L1) complexes get square–planar and tetrahedral geometries and the complexes oflig and (L2) get an octahedral geometry. Antimicrobial examinations show good results in the sharing complexes.
The molecular structures of acetophenonylidine-4-aminopyridine (I), 2, 6-dihydroxyacetophenonlidine-4-aminopyridine (II), 2, 4, 6- trihydroxyaceto phenonylidine-4-aminopyridine (III) and 2, 6-dihydroxyacetophenonylidine-2-aminopyridine (IV) have been investigated by IR and UV-visible spectrophotometry. The IR data indicate that the hydroxyl groups of these Schiff bases exist as tautomeric mixtures of free and bonded with the azomethine groups. The electronic spectra, effect of polar and nonpolar solvents, and the effect of acidity and basicity on the electronic spectra were studied and discussed. Their charge-transfer (CT) complexes with chloranil in chloroform solvent were also investigated; these complexes absorb light at 398-533 nm. T
... Show MoreSeveral new derivatives of 1,3,4-oxadiazoles and 1,2,4-triazoles linked to 3,4,5,6-tetrachlorophthalimide moiety were synthesized through following multisteps. The first step involved preparation of 3,4,5,6-tetrachlorophthalimide via reaction of 3,4,5,6-tetrachlorophthalic anhydride with urea at high temperature. Treatment of the resulted imide with ethyl chloroacetate in the second step afforded tetrachlorophthalimidyl ester which inturn was introduced in reaction with hydrazine hydrate in the third step, producing the corresponding acetohydrazide. The synthesized acetohydrazide was introduced in different synthetic paths including treatment with phenyl isothiocyanate or reaction with carbon disulfide in alkaline solution then with hydr
... Show MoreThe compound [G1] was prepared from the reaction of thiosemicarbazide with para-hydroxyphenylmethyl ketone in ethanol as a solvent. Then by sequence reactions prepared [G2] and [G3] compounds. The compound [G4] reaction with ethyl acetoacetoneto synthesized compound [G6] and acetyl acetone to synthesized compound [G5]. Reaction the [G3] with two different types of aldehydes in the present of pipredine to form new alkenes compounds [G7]and [G8].The compound [G3] reacted with hydrazine hydrate to formation[G4] with present the hydrazine hydrade 80% in (10) ml of absolute ethanol. Latter the compound [G4]reacted with different aldehydes with present the glacial acetic acid and the solvent was ethanol to formed the Schiff bases compounds[G9] an
... Show MoreThe compound [G1] was prepared from the reaction of thiosemicarbazide with para-hydroxyphenylmethyl ketone in ethanol as a solvent. Then by sequence reactions prepared [G2] and [G3] compounds. The compound [G4] reaction with ethyl acetoacetoneto synthesized compound [G6] and acetyl acetone to synthesized compound [G5]. Reaction the [G3] with two different types of aldehydes in the present of pipredine to form new alkenes compounds [G7]and [G8].The compound [G3] reacted with hydrazine hydrate to formation[G4] with present the hydrazine hydrade 80% in (10) ml of absolute ethanol. Latter the compound [G4]reacted with different aldehydes with present the glacial acetic acid and the solvent was ethanol to formed the Schiff bases compounds[G9] an
... Show MoreTo 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
... Show MoreBacterial infections pose an ongoing challenge due to resistance developed by infectious bacteria. So much research targeting designing new antibacterials is published annually. Our goal is to synthesize compounds that have given antibacterial activity according to molecular docking against the chosen target protein and that have acceptable ADMET properties that can be synthesized and used in the future. New 2-(5-methoxy-1-(4-chlorobenzene)-2-methyl-1H-indol-3-yl)acetohydrazide derivatives’ antibacterial efficacy against two common strains of Gram-negative and Gram-positive microorganisms has been developed, produced, and investigated. Sophisticated, modern analytical methods, including ATR-FTIR and 1H NMR spectroscopy, were used
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