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Synthesis and Characterization of some new heterocyclic derivatives from aromatic carbonyl ‎compounds and carboxylic acids with Evaluation some of them for biological activity
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     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.

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Publication Date
Sat Mar 30 2019
Journal Name
Studia Universitatis Babeș-bolyai Chemia
"Excess and deviations properties for the binary solvent mixtures of tetrahydrofurfuryl alcohol with some aromatic hydrocarbons at 298.15K "
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Publication Date
Sun Jun 05 2016
Journal Name
Baghdad Science Journal
Synthesis, Characterization of Derivatives Tetrazoles for Trimethoprim Drug
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The present work involved synthesis of serval new substituted tetrazole via Schiff bases for trimethoprim drug by two steps. The first step involved direct reaction of different ketones and aldehydes with trimethoprim producing the corresponding Schiff bases (1-10), whereas the second step, involved preparation new tetrazoles derivatives (11-20) through reaction of the ready Schiff bases (in the first step) with sodium azidein in dioxin. The prepared compounds were characterized by UV, FT-IR, and some of them by 13C-NMR, 1H-NMR spectroscopy and physical properties.

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Publication Date
Sun Apr 14 2019
Journal Name
International Journal Of Pharmaceutical Research
Synthesis, Characterization and Antibacterial of Some New 4,4-(pyridine-2,6-diylbis(1,3,4-oxadiazole-5,2-diyl))bisphenol Polymer
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4, 4s (pyridine 2, 6 diylbis (1, 3, 4 oxadiazole 5, 2 diyl)) bisphenol monomer (3) was synthesized from cyclization of Ns2, Ns6 bis (4 hydroxybenzylidene) pyridine 2, 6 dicarbohydrazide (2) in the presence of bromine in glacialacetic acid. Newly five polymers (P1P5) were synthesized from reaction bis 1, 3, 4 oxadiazole bisphenolmonomer with five different di acid chloride. The antibacterial activity of the synthesized polymers was screened against gram positive and gram negative bacteria. Polymers P4 and P5 exhibited significant antibacterial against all microorganisms, as well these polymers showed highest antifungal activity.

Publication Date
Fri Nov 01 2024
Journal Name
Current Medicinal Chemistry
Synthesis, In Silico Prediction, and In Vitro Evaluation of Anti-tumor Activities of Novel 4'-Hydroxybiphenyl-4-carboxylic Acid Derivatives as EGFR Allosteric Site Inhibitors
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Introduction:

Allosteric inhibition of EGFR tyrosine kinase (TK) is currently among the most attractive approaches for designing and developing anti-cancer drugs to avoid chemoresistance exhibited by clinically approved ATP-competitive inhibitors. The current work aimed to synthesize new biphenyl-containing derivatives that were predicted to act as EGFR TK allosteric site inhibitors based on molecular docking studies.

Methods:

A new series of 4'-hydroxybiphenyl-4-carboxylic acid derivatives, including hydrazine-1-carbothioamide (S3-S6) and 1,2,4-triazole (S7-S10) derivatives, were synthesized and characterized using IR, 1HNMR, 13CNMR

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Publication Date
Sat Nov 04 2023
Journal Name
Iraqi Journal Of Pharmaceutical Sciences( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis and Preliminary Anti-Inflammatory and Anti-Microbial Evaluation of New 4,5-Dihydro-1H-Pyrazole Derivatives
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Abstract      Organic compounds with pyrazole cores have a variety of uses, notably in the pharmaceutical and agrochemical sectors. The interest in creating pyrazole compounds, examining their many features, and looking for potential uses is growing. Our work has concert with synthesis of  chalcones and pyrazolines, then finally pyrazoline-aniline derivatives and evaluation their anti-inflammatory, antibacterial and antifungal activities

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Publication Date
Wed Aug 28 2019
Journal Name
Revista Aus
Synthesis and Identification of New Derivative of L-ascorbic Acid with Glycine and Some Metal Complexes
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The reaction of starting materials (L-asCl2):bis[O,O-2,3;O,O-5,6-(chloro(carboxylic) methylidene)]- -L-ascorbic acid] with glycine gives new product bis[O,O-2,3,O,O-5,6-(N,O-di carboxylic methylidene N-glycine)-L-ascorbic acid] (L-as-gly) which is isolated and characterized by, Mass spectrum UV-visible and Fourier transform infrared spectrophotometer (FT-IR) . The reaction of the (L-as-gly) with M+2; Co(II) Ni(II) Cu(II) and Zn(II) has been characterized by FT- IR , Uv-Visible , electrical conductivity, magnetic susceptibility methods and atomic absorption and molar ratio . The analysis showed that the ligand coordinate with metal ions through mono dentate carboxylic resulting in six-coordinated with Co(II) Ni(II) Cu(II) ions while with

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Publication Date
Fri Feb 28 2025
Journal Name
Moroccan Journal Of Chemistry
Design, Synthesis, and Biological Evaluation of new sulfonamides derived from 2-Aminopyridine: Molecular docking, POM analysis, and identification of the pharmacophore sites
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New series of imidazole[1,2-a]pyridine-sulfonamides was designed and synthesized from 2-aminopyridine, which was reacted with p-bromo phenacyl bromide in the present of MgO to produce the corresponding imidazole[1,2-a]pyridine, which was then reacted with chlorosulfonic acid to produce 2-(4-bromophenyl)imidazole[1,2-a]pyridine-3-sulfonyl chloride [2]. Following that, treatment of (2) with different amines using the grand method to generate imidazole [1,2-a] pyridine sulfonamides. All the synthesized compounds have been characterized by FTIR, 1HNMR and 13CNMR and C.H.N analysis. The DFT, POM analysis and molecular docking were carried out on for all final compounds to investigate drug like attributes, and the results revealed showed that the

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Publication Date
Fri Mar 01 2013
Journal Name
Al-nahrain Journal Of Science
Synthetic and Characterization of Some new Schiff bases Complexes with CoII, NiII, CuII and PdII ions
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A new ligand (H4L) and its complexes with (CoII, NiII, CuII and PdII). This ligand was prepared in two steps, in the first step a solution of terephthaldehyde in methanol reacted under refluxe with 1,2-phenylenediamine to give precursore compound which reacted in the second step with 2,4- dihydroxybenzaldehyde to give the ligand. The complexes were synthesized by direct reaction of the corresponding metal chloride with the ligand. The ligand and complexes were characterized by spectroscopic methods [FT-IR, UV-vis, 1HNMR, HPLC and atomic absorption], chloride contant in addition to conductivity measurement. The stability constant K and Gibbs free energy ∆G were calculated for [[Ni2(H2L)Cl2], [Cu2(H2L)Cl2] complexes using spectrophoto

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Publication Date
Mon May 08 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Synthesis And Characterization Of New Oxazepines Derived From D-Erythroascorbic Acid
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 The new schiff bases derived from D-erythroascorbic acid contaning heterocyclic unit were synthesized by condensation of D-erythroascorbic acid with aromatic amine (containing 1,3,4oxadiazole or 1,3,4-thiadiazole unit) in dry benzene using glacial acetic acid as a catalyst.  Derythroascorbic acid [IV] was synthesized by four steps (Scheme 1), while the primary aromatic amine which is containing 1,3,4-oxadiazole [VII] or 1,3,4-thiadiazole [VIII] synthesized by the reaction of 4methoxy benzoyle hydrazine [VI] with 4-amino benzoic acid or by the reaction  tuloic acid with thiosemicarbazide, respectively in the presence of POCl3. The new  1,3-oxazepine derivatives were obtained by addition reaction of Schiff bases with d

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Publication Date
Tue Sep 01 2020
Journal Name
Biochemical And Cellular Archives
SYNTHESIS, SPECTRAL AND THERMAL CHARACTERIZATION OF NI(II), CU(II) AND ZN(II) COMPLEXES WITH NEW LIGAND TOWARDS POTENTIAL BIOLOGICAL APPLICATION
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Series of new complexes of the type [M2 (L)Cl4 ] are prepared from the new ligand[N1 ,N4 -bis(benzo[d]thiazol-2- yl)succinamide (L) derived from ethan-1,2-dicarbonyl chloride and 2-aminobenzothiozole,where, M= Ni(ii), Cu(ii) and Zn(ii) alsocomplexes of mix-ligands, the type [M(L)(8-HQ)]Cl, where, M = Ni(ii), Cu(ii) and Zn(ii),8-HQ= 8-Hydroxyquinoline. Chemical forms are obtained from their 1 H, 13CNMR, Mass spectra (for (L)), FT-IR and U.V spectrum, melting point, molar conduct.Using flame (AA), % M is determined in the complexes.The content of C, H, N and S in the (L) and its complexes was specified. Magnetic susceptibility and thermal analysis (TGA) of prepared compounds were measured.The propose geometry for all complexes[M2 (L)Cl4 ] wa

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