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Synthesis and Characterization of Some New Pyridine and Pyrimidine Derivatives and Studying Their Biological Activities
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Heterocyclic systems, which are essential in medicinal chemistry due to their promising cytotoxic activity, are one of the most important families of organic molecules found in nature or produced in the laboratory. As a result of coupling N-(4-nitrophenyl)-3-oxo-butanamide (3) using thiourea, indole-3-carboxaldehyde, or piperonal, the pyrimidine derivatives (5a and 5b) were produced. Furthermore, pyrimidine 9 was synthesized by reacting thiophene-2-carboxaldehyde with ethyl cyanoacetate and urea with potassium carbonate as a catalyst. The chalcones 11a and 11b were synthesized by reacting equal molar quantities of 1-naphthaldehyde and 2-quinoline carboxaldehyde with 4-Bromo acetophenone and 4- fluoro acetophenone respectively. Pyrimidine 13 was synthesized by reacting chalcone 11a with guanidine hydrochloride in the presence of potassium hydroxide. Pyridine derivative 14 was prepared from the reaction of chalcone 11b with ethyl cyanoacetate and ammonium acetate in glacial acetic acid. In addition, the reaction of 4-methyl benzaldehyde and 4-fluoro acetophenone with ethyl cyanoacetate and ammonium acetate in n-butanol gave pyridine derivative 16. Spectral investigations (FT-IR, 1H, and 13C-NMR) and EI-MS spectra were used to determine the structure of the prepared compounds. The synthesized derivatives were tested in vitro for their potential cytotoxicity against two different human cancer cell types, MCF-7 (breast cancer cell) or HepG2 (liver cancer cell). Compounds 5a and 14 displayed cytotoxic activity versus HepG2 cell line with IC50 values of 43.84 and 57.14 µg /mL, respectively. Furthermore, the pyridine compound 14 demonstrated cytotoxic action versus MCF-7 with an IC50 value of 50.84 g/mL. The antibacterial and anti-parasitic properties of the synthesized derivatives have also been described.

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Publication Date
Tue Dec 05 2023
Journal Name
Baghdad Science Journal
Synthesis and Antibacterial Evaluation for Some New Schiff-bases Derived from P-aminoacetanilide
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Derivatives of Schiff-bases possess a great importance in pharmaceutical chemistry. They can be used for synthesizing different types of bioactive compounds. In this paper, derivatives of new Schiff bases have been synthesized from several serial steps. The acid (I) was synthesized from the reaction of dichloroethanoic acid with 2 moles of p-aminoacetanilide. New acid (I) converted to its ester (II) via the reaction of (I) with dimethyl sulphate in the present of anhydrous of sodium carbonate and dry acetone. Acid hydrazide (III) has been synthesized by adding 80% of hydrazine hydrate  to the new ester using ethanol as a solvent. The last step included the preparation of new Schiff-bases (IV-VIII) by the reaction of acid hydrazide with app

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Publication Date
Tue Nov 20 2018
Journal Name
Research Journal Of Pharmaceutical, Biological And Chemical Sciences
Synthesis, Characterization And Microbial Efficiency Of Azo Dye Ligand Complexes With Some Metal Ions
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4-[(2-hydroxy-4,6-dimethylphenyl)diazenyl]-1,5-dimethyl-2-phenyl-1H-pyrazol-3(2H)-one has been readied by combination the diazonium salt of 4-aminoantipyrine with 3,5-dimethylphenol. Spectral studies ( FTIR, UV-Vis, 1H and 13CNMR) and microelemental analysis (C.H.N) are use to identified of the ligand. Complexes of some transition metals were performed as well depicted. The formation of complexes were characterized by using atomic absorption of flame, elemental analysis, infrared and UV-Vis spectral process as well conductivity and magnetic quantifications. Nature of compounds produced have been studied followed the mole ratio and continuous contrast methods, Beer's law followed during a concentration scope (1×10-4 - 3×10-4 M/L). height m

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Publication Date
Sun Dec 20 2020
Journal Name
Journal Of Global Pharma Technology
Synthesis, Characterization, Antibacterial and Antifungal Activity of Some Bis (1, 3, 4-oxadiazole) Polymer
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Pyridine-2, 6-dicarbohydrazide comp (2) was synthesized from ethanolic solution of diethyl pyridine-2, 6- dicarboxylate comp (1) with excess of hydrazine hydrate. Newly five polymers (P1-P5) were synthesized from reaction of pyridine-2, 6-dicarbohydrazide comp (2) with five different di carboxylic acid in the presence of poly phosphoric acid (PPA). The antibacterial activity of the synthesized polymers was screened against some gram positive and gram negative bacteria. Antifungal activity of these polymers was evaluated in vitro against some yeast like fungi such as albicans (candida albicans). Polymers P3, P4 and P5 exhibited highest antibacterial and antifungal against all microorganisms under test.

Publication Date
Sun Jun 25 2023
Journal Name
International Journal Of Drug Delivery Technology
Synthesis, Characterization, Antimicrobial and Antioxidant Study of New Complexes Schiff Base Derived from 2, 5-diChloroaniline
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Metal complexes of Mn(II), Co(II), Ni(II), Cu(II), Cd(II), Zn(II), Hg(II), Pd(II), and Pt(II) with Schiff base ligand (LH) derived from 2,5-dichloroaniline and 2-hydroxy-5-metheylbenzalaldehyde were synthesized and characterized using a variety of spectrophotometric techniques The findings of the spectroscopic analysis indicated that (LH) behaved as a binary coordinating agent to the metal ion by the N and O atoms, and the geometry shape of the complexes was octahedral, with the exception of the Pd and Pt complexes, which had a square planar geometry. Using the DPPH radical scavenging method, we investigated the antimicrobial activity of the compound against Staphylococcus aureus and Escherichia coli, as well as the antifungal activity of t

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Publication Date
Sun Jun 13 2021
Journal Name
International Journal Of Drug Delivery Technology
Synthesis, Characterization and Anticorrosion Studies of New Co(II), Ni(II), Cu(II), and Zn(II) Schiff Base Complexes
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The research included preparation of new Schiff base (L) by two steps: preparation of precursor [bis(2-formyl-6-methoxyphenyl) succinate] (P) by reacting (3-methoxy salicyl aldehyde) with (succinoyl dichloride) as first step then react the prepared precursor (P) with (ethanethioamide) to have the new Schiff base [bis(2-((ethane thioyl imino) methyl)-6-methoxy phenyl) succinate] (L) as second step. Characterized compounds based on Mass spectra, 1 H, 13CNMR (for ligand (L)), FT-IR and UV spectrum, melting point, molar conduct, %C, %H, and %N, the percentage of the metal in complexes %M, magnetic susceptibility, while study corrosion inhibition (mild steel) in acid solution by weight loss. These measurements proved that by (Oxygen, Nitrogen, a

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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
Wed Jul 01 2015
Journal Name
Journal Of Saudi Chemical Society
Synthesis, characterization and comparative study the microbial activity of some heterocyclic compounds containing oxazole and benzothiazole moieties
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Publication Date
Tue Apr 01 2014
Journal Name
Structural Science, Crystal Engineering And Materials
Comparison of the structural motifs and packing arrangements of six novel derivatives and one polymorph of 2-(1-phenyl-1H-1,2,3-triazol-4-yl)pyridine
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The crystal structures of a new polymorph and seven new derivatives of 2-(1-phenyl-1H-1,2,3-triazol-4-yl)pyridine have been characterized and examined along with three structures from the literature to identify trends in their intermolecular contact patterns and packing arrangements in order to develop an insight into the crystallization behaviour of this class of compound. Seven unique C-H...X contacts were identified in the structures and three of these are present in four or more structures, indicating that these are reliable supramolecular synthons. Analysis of the packing arrangements of the molecules using XPac identified two closely related supramolecular constructs that are present in eight of the 11 structures; in all cases, the st

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Publication Date
Tue Feb 01 2022
Journal Name
Baghdad Science Journal
New White Method of Parameters and Reliability Estimation for Transmuted Power Function Distribution
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        In this paper, an estimate has been made for parameters and the reliability function for Transmuted power function (TPF) distribution through using some estimation methods as proposed new technique for white, percentile, least square, weighted least square and modification moment methods. A simulation was used to generate random data that follow the (TPF) distribution on three experiments (E1 , E2 , E3)  of the real values of the parameters, and with sample size (n=10,25,50 and 100) and iteration samples (N=1000), and taking reliability times (0< t < 0) . Comparisons have been made between the obtained results from the estimators using mean square error (MSE). The results showed the

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Publication Date
Sun Jan 01 2023
Journal Name
2nd International Conference On Mathematical Techniques And Applications: Icmta2021
Antimicrobial activities of some new heterocyclic compounds bearing imidazo[2,1-b]benzothiazole moiety
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