Many new heterocyclic compounds including 4-thiazolidinones containing indole with triazole units were described. The new Schiff bases [VII]a, b and [VIII]a,b synthesized by condensation acid hydrazides [II],[VI] with different (aromatic) aldehydes in absolute ethanol. The refluxing equimolar amounts of the Schiff bases ([VII]a,b, [VIII]a,b) with thioglycolic acid in benzene led to get thiazolidin-4-ones derivatives ([IX]a,b and [X]a-d). Finally, the new derivatives [XI]a-c run out via the reacted compound [IX]a with different n-alkyl bromide (methyl bromide, ethyl bromide, and butyl bromide) in alkaline media.
The synthesized ligand (3-(2-amino-5-(3,4,5-tri-methoxybenzyl)pyrimidin-4-ylamino)-5,5-dimethylcyclohex-2-enone] [H1L1] was characterized via fourier transform infrared spectroscopy (FTIR), 1H, 13C – NMR, Mass spectra, (CHN analysis), UV-vis spectroscopic approaches. Analytical and spectroscopic techniques like chloride content, micro-analysis, magnetic susceptibility UV-visible, conductance, and FTIR spectra were used to identify mixed ligand complexes. Its (ML13ph) mixed ligand complexes [M= Co (II), Ni (II), Cu (II), Zn (II), and Cd (II); (H1L1) = β-enaminone ligand=L1 and (3ph) =3-aminophenol= L2]. The results demonstrate that the complexes are produced with a molar ratio of M: L1:L2 (1:1:1). To generate the appropriate compl
... Show MoreObjective: Benzoxazole derivatives have antifungal, anticancer, antibacterial, and anticonvulsant function. Encouraged by this comment, we agreed to synthesize new Benzoxazole compounds connected to the bases of Schiff's. Methods: 2,4-diaminophenol (1) was prepared by the reaction of 2,4-dinitrophenol and sodium dithionate. Compound (1) reacted with either acetic acid to afford compound (2) or with formic acid to afford compound (3). The Schiff bases were preparation from the reaction condensing reaction of compound (2) or (3) and aromatic aldehydes or ketone; [p-nitrobenzaldehyde, p-hydroxybenzaldehyde, p-chlorobenzaldehyde, p-bromoacetophenone and terephthaldehyde]. Results: FTIR and 1H-NMR spectroscopy characterized all of the pr
... Show MoreFour batches of sertraline HCl microspheres were prepared using a poly (D-L-lactide-co-glycolide) (PLGA) polymer ( Mw. 9, 27, 30 and 83 KDa) as a delivery system. The microspheres were prepared by a dispersion/solvent extraction-evaporation method and characterized for drug loading by UV, particle size by laser diffractometry and surface morphology by scanning electron microscopy (SEM). The in vitro sertraline HCl release was studied. Spherical microspheres with a mean diameter of 21 to 26 µm loaded with 24.6 – 38.2% were produced. The in vitro drug release was shown to be depend on polymer molecular weight and also on the drug loading. Differential scanning calorimetry (DSC) was employed to investigate the physical state
... Show MoreObjective: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 MoreThe 3-aminoacetophenone and 4-aminoantipyrine were used as precursors to prepare new six ligands. The three new ligands (L1,L2 and L3) were synthesis by reacting one mole of 3-aminoacetophenone with one mole of (Acetyl chloride), (benzoyl chloride), (4-methoxybenzoyl chloride) and ammonium thiocyanat in acetone as a solvent, they are:- L1 (AAA) =[N-(3-acetylphenylcarbamothioyl)acetamide] L2 (BAA) =[N-(3-acetylphenylcarbamothioyl)benzamide] L3 (MAA) =[N-(3-acetylphenylcarbamothioyl)-4-methoxy benzamide] Also three new derivatives of 4-aminoantipyrine were synthesis by reacting one mole of 4-aminoantipyrine with one mole of (Acetyl chloride), (benzoyl chloride), (4-methoxybenzoyl chloride) and ammonium thio
... Show MoreWith the study of synthesizing new organic compounds and exploring biological potency. Aryldiazenyl derivatives (2-5) were carried out by coupling of diazonium salt of 4-aminoacetophenone (1) and miscellaneous active methylene compounds such as: acetylacetone, ethyl cyanoacetate, dimedone or methyl acetoacetate. Moreover substituted 1,2,3-triazole (7-9) were synthesized by the cyclization of 1-(4-azidophenyl) ethanone (6); (which was obtained by coupling of diazonium salt (1) with sodium azid); with acetylacetone, methyl acetoacetate or methyl cyanoacetate, respectively. The structures of the prepared compounds were promoted by IR, H1NMR and UV/Visible spectra. Further, they were examined in vetro for antibacterial activity against five str
... Show MoreFive derivatives of thiadiazole were prepared with aldehydes and alkyl halides, compoundA: 2-amino-5-thiol-1,3,4- thiadiazole, compound B :2-(o-hydroxybenzylidine)amino-5-thiol-1,3,4-thiadiazole, compoundC: 2(2-butan-lidine)amino-5-thiol-1,3,4-thiadiazole, compound E: 2- amino-5-(2-Propanylthio)-1,3,4-thiadiazol) and compound F:2(o-chlorobenzylamino)-5-(2-propanyl thio)-1,3,4 thiadiazol. All prepared compounds were diagnosed by (IR) and (UV) Spectroscopy. All of those compounds were screened for their anti-microbial activity in vitro. The results show that most of the compounds A, B, C exhibited moderate to good activity against Gram-positive bacteria and the same compound exhibit low to moderate activity on most gram-negative bacte
... 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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