In this research investigation, a total of eighteen diverse tetra- and penta-lateral cyclic compounds were synthesized. These included 1,3,4-thiadiazole, thiazolidin-4-one (via an alternative method), 1,2,4-triazole, carbothioamide, thiazole-4-one, azetidin-2-one, and oxazole. The synthesis procedure entailed a sequence of reactions. The thiazolidine-4-one 1 was obtained by reaction p-aminobenzoic acid with thiosemicarbazide, followed by treatment with p-tolualdehyde to produce Schiff base 2. Reaction Schiff base 2 with mercaptoacetic acid in dry benzene was carried out to produce thiazolidine-4-one 3. In another synthesis pathway, the esterification of p-nitro benzoic acid with ethanol in the presence of sulfuric acid was obtained to formation of compound 4. Compound 4 was subsequently reacted with thiosemicarbazide, yielding compound 5. Cyclization of compound 5 was then achieved using 4% sodium hydroxide solution. This formed the 1,2,4-triazole heterocycle, designated compound 6. Thiosemicarbazone 7-9 were prepared by reaction of thiosemicarbazide with different aldehydes. Additionally, 2-substituted-1,3-thiazolidine-4-one derivatives 10-12 were synthesized through the reaction of thiosemicarbazone with chloroacetic acid in the presence of anhydrous sodium acetate. The Oxazole derivative 15 was obtained through a series of reactions starting with the reaction of p-amino benzoic acid with ethyl chloroacetate, resulting in compound 13. Compound 13 was then treated with urea to obtain compound 14, followed by a reaction with 4-phenyl phenacyl bromide to yield the final product, the Oxazole derivative 15. The 2-aminooxadiazole derivative 16 was synthesized by reaction urea with 4-bromoacetophenone which was reacted with 4-bromobenzaldehyde to produce Schiff base derivative 17. Finally, β-lactam 18 is obtained through reaction Schiff base with chloroacetyl chloride in the presence of triethyl amine. FT-IR, 1H-NMR, and 13C-NMR spectroscopy were used to confirm their proposed structures. Moreover, the antibacterial and antifungal activities of certain synthesized compounds, specifically 2,3,6,11,13,15,17, and 18, were assessed against Staphylococcus aureus, Escherichia coli, and Candida albicans, demonstrating encouraging outcomes.Keywords: Antibacterial, antifungal activity, oxadaizole, heterocyclic derivatives, Oxazole.
A series of Schiff base-bearing salicylaldehyde moiety compounds (1-4) had been designed, synthesized, subjected to insilico ADMET prediction, molecular docking, characterization by FT-IR, and CHNS analysis techniques, and finally to their Anti-inflammatory profile using cyclooxygenase fluorescence inhibitor screening assay methods along with standard drugs, celecoxib, and diclofenac. The ADMET studies were used to predict which compounds would be suitable for oral administration, as well as absorption sites, bioavailability, TPSA, and drug likeness. According to the results of ADME data, all of the produced chemicals can be absorbed through the GIT and have passed Lipinski’s rule of five. Through molecular docking with PyRx 0.8, these
... 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 MoreThis paper presents the synthesis and study of some new mixed-ligand complexes containing nicotinamide(C6H7N2O) symbolized (NA) and phenylalanine (C9H11NO2)symbolized (pheH)] with some metal ions. The resulting products were found to be solid crystalline complexes which have been characterized by :Melting points, Solubility, Molar conductivity. determination the percentage of the metal in the complexes by flame(AAS), magnetic susceptipibility, Spectroscopic Method [FT-IR and UV-Vis]. The proposed structure of the complexes using program , chem office 3D(2006) . The general formula have been given for the prepared complexes : [M(NA)2(phe)]cl M(II): Mn(II) ,Co(II) , Ni(II) , Cu(II) , Zn(II) , Cd(II) & Hg(II)). NA = Nicotinamide= C6
... Show MoreThis paper presents the synthesis and study of some new mixed-liagnd complexes containing nicotinamide(C6H7N2O) symbolized (NA) and phenylalanine (C9H11NO2)symbolized (pheH)] with some metal ions. The resulting products were found to be solid crystalline complexes which have been characterized by :Melting points, Solubility, Molar conductivity. determination the percentage of the metal in the complexes by flame(AAS), magnetic susceptipibility, Spectroscopic Method [FT-IR and UV-Vis]. The proposed structure of the complexes using program , chem office 3D(2006) . The general formula have been given for the prepared complexes :[M(NA)2(phe)]cl M(II): Mn(II) ,Co(II) , Ni(II) , Cu(II) , Zn(II) , Cd(II) & Hg(II) . NA = Nicotinamide= C6H7N2O Phe -
... Show MoreA new ligand [3(3(2chloroacetyl) thioureido)pyrazine-2-carboxyliIcacid](CPC)was synthesized by reaction of rized by imicro elmental analysis C.H.N.S.,FT-IR,UV-Vis and 1H-13CNMR spectra, some transition metals complex ofIthis ligand were Prepared and characterized byiFT-IR,UV-Vis spectra conductivity measurements magnetic susceptibility and atomic absorption. From the obtained results the molecular formula of all prepared complexes were[M(CPC)2](M+2i=Mn. Co, Ni, Cu, Zn, Cd and Hg),the proposedi geometrical structure for all complexes were as tetrahedral geometry except copper complex has square planer geometry.
A series of coumarin derivatives linked to amino acid ester side chains were synthesized and evaluated of their antibacterial and antifungal activity. The coumarin derivatives was alkylated by the ethyl bromoacetate and then using potassium carbonate to get alkylated hymecromone. Conventional solution method for amide bond formation was used as a coupling method between the carboxy-protected amino acids with acetic acid side chain of coumarin derivatives. The DCC/ HOBt coupling reagents were used for peptide bond formation. The proposed analogues were successfully synthesized and their structural formulas were consistent with the proposed struct
... Show MoreMany condensed polymers [A1-A7] were prepared via reaction of (Ethylenediaminetetraacetic acid = EDTA), with different prepared imide-diamines by modification [ modification of amino acids and antibiotics (B1- B7)] Imide-diamines were prepared by chlorination of L-amino acids such as [ L-Histidine, L-Alanine, L-Valine, L-Glycine and L-Aspargine ] or selected antibiotics such as [Cephallixine monohydrate and Amoxilline ] with thionyl chloride at 0°C, then reacted with ammonia to obtain imidediamines [B1-B7] . The physical properties of all prepared condensed polymers [A1-A7], new prepared diamines [B1-B7] were studied and characterized by FT -IR spectroscope to certify the structural formulas. The thermal analysis (TGA, DTA) were studied, a
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