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 synthesized Schiff bases 3 (ac) and 4 (ac) were examined for their in vitro antimicrobial activity using different Gram-positive bacteria, Gram-negative bacteria, and Candida albicans as fungi. The obtained results were compared with standard drugs: amoxicillin, ciprofloxacin, and fluconazole. All the compounds show no antifungal activity at any concentrations used, while most of them show moderate antibacterial activity at concentration 5mg/mL toward most bacteria except Klebsiella pneumonia.
Condensation of 4-methoxybenzoyl hydrazine with 4- aminobenzoic acid in the presence of POCl3 gave the oxadiazole derivative [III] .This compound was demethylated with aluminium chloride to give series of 2- (4-hydroxy phenyl)-5-(4-amino phenyl)
1,3,4-oxadiazole [IV]. Series of Schiff s bases [V]n were synthesized by the condensation of compound [IV] with 4-n-alkoxy benzaldehyde in the presence of glacial acetic acid. Condensation of compounds [VI]n. with adipoyl chloride in dry pyridine leads to the formation of a new homologous series [VI]n. The structures of the synthesized compounds were confirmed by physical and spectral means The new compounds [VI]n have been screened for their antibacterial activities . The results
A new Schiff base of HL has been synthesized from amoxicillin drug and 4- Chlorobenzophenone. Cr (III), Fe (III), Co (II), Ni (II), Cu (II), Cd (II) and Hg (II) mixed ligands complexes of Schiff base and Nicotinamide. Diagnosis of synthesis ligand and its complexes are done by 1HNMR, 13CNMR and thermal analysis for HL ligand, FTIR, UV-visible, molar conductance, CHN analysis, magnetic susceptility and atomic absorption. Octahedral geometries have been suggested for all complexes. All compounds under study were tested antimicrobial activity against four type of bacteria such as Pseudomonas aeruginosa, Escherichia coli, Staphylococcus aureus Bacillis subtilis in nutrient agar.
This research included the preparation of 2-mercaptobenzoxazole (N1) by the reaction of ortho-aminophenol with carbon disulfide in an alcoholic potassium hydroxide solution. The 2-mercapto benzoxazole (N1) was then treated with hydrazine to obtain the 2-hydrazino benzoxazole (N2). A number of hydrazones (N3-N5) were prepared through the reaction of N2 with different benzaldehydes. The compound (N6) was also prepared whereby the ring closing of hydrazone (N3) using chloroacetylchloride, while the compound (N7) was prepared by treating 2-hydrazino benzoxazole with acetylacetone. When the compound (N1) was treated with formaldehyde, it afforded the compound (N8). Also, the N9 was obtained from the reaction of N1 with chloroacetic acid in th
... Show Moren this study new derivatives of Schiff bases (5-10) were synthesized from the new starting material 1 . Which has been synthesized by the reaction of (1 mol.) of dichloroacetic acid with two moles of morpholine, in the presence of potassium hydroxide, Ester derivatives 2 and 3 were synthesized by the reaction of 1 with methanol or ethanol respectively in the presence of sulphuric acid as catalyst . Compound 2 was also prepared from dimethylsulphate with high yield , 2 and 3 was used to synthesized 2,2-dimorpholinylacetohydrazide 4 via reaction with NH2NH2.H2O 80% .Imines (5-10) were synthesized via the reaction of 4 with appropriate aromatic aldehydes in the presence of G.A.A as a catalyst . Derivatives compounds (1-10) were identifie
... Show MoreObjective: This study involved the synthesis of new Schiff bases and 1,3-oxazepine derivatives from the baclofen drug and study the anticancer activities. Methods: Baclofen was initially reacted with aromatic aldehydes to create Schiff base derivatives (Ia–Ib), which were then closed in the next step using anhydrous acids to form oxazepine derivatives (IIa–IId). Results: The title compounds were synthesized successfully and identified using FT-IR, 1H NMR, and 13C NMR spectroscopy. Additionally, compound (IIc)’s (3-(4-chloro-phenyl)-4-[2-(4nitro-phenyl)-4,7-dioxo-4,7-dihydro-[1,3] oxazepin-3-yl]butyric acid) anticancer activity was assessed using MTT assay against FTC-133 (thyroid cancer) compared with WRL-68 (normal cell line). Discus
... Show MoreThe work involves synthesis of new Schiff bases ( [V]a, b and [VI]a, b), pyrazoles[VII]a, b and pyrazolines[VIII]a, b derivatives containing isoxazoline unit starting with chalcones. 4bromoacetophenone was reacted with 4-hydroxybenzaldehyde or 4-hydroxyacetophenone was reacted with 4-bromobenzaldehyde in basic medium to give chalcone by Claisen-Schemidt reaction. The chalcons [I]a, b was reacted with hydroxylamine hydrochloride to form isoxazolines [II]a, b. which were reacted with ethyl chloro acetate in basic medium to get ester compounds[III]a, b .The condensation new ester[III]a, b with hydrazine hydrate80% yieldedacid hydrazide [IV]a, b.The later compound refluxing with 4-substituted benzaldehyde in dry benzene to
... Show MoreCoumarin derivatives have shown different biological activities, such as antifungal, antibacterial antiinflammatory, and antioxidant activities, besides antibiotic resistance modulating effects, and anti-HIV, hepatoprotective, and antitumor effect. So, new coumarin derivatives (hydrazones and an amide) were synthesized through multisteps reactions. All the synthesized target compounds were characterized by FT-IR spectroscopy, 1HNMR analysis. The compounds then evaluated for their anti-bacterial activity by means of well-diffusion method against two gram-positive bacteria (Staphylococcus aureus, Streptococcus pneumoniae) and two gram-negative bacteria (E.coli and Pseudomonas aeruginosa). The highest activity was demonstr
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