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Synthesis, characterization and biological evaluation of new potentially active hydrazones of naproxen hydrazide
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To synthesize new hydrazone derivatives of naproxen with enhanced anti-inflammatory activity and devoid the ulcerogenic side effects. Hydrazones were synthesized by conjugation of naproxen hydrazide with seven natural and synthetic aldehyde and ketone by using glacial acetic acid as catalyst. The synthesis has been carried out following simple methodology in excellent isolated yields.The structure of the synthesized derivatives has been characterized by elemental microanalysis (CHN), FTIR Spectroscopy, and other physicochemical properties.The anti- inflammatory activity of the synthesized compounds was evaluated in vivo using the egg-white induced edema model in rats, and the results of the biological assay was found to be comparable to Naproxen in this regard. The synthesizedhydrazone of naproxen hydrazides with their pronounced anti-inflammatory activity can enhance the anti-inflammatory activity of naproxen to a varying degree according to the type of aldehyde or ketone used.

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Publication Date
Mon Jun 03 2024
Journal Name
Journal Of Kufa For Chemical Sciences
Synthesis and Preliminary Biological study of New Chalcone Derivatives Containing Isoxazoline Moiety
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                          In this research work, synthesis, antimicrobial and antioxidant bioactivity of a chain of compounds having unsaturated ketones bond and isoxazoline moiety have been described. New chalcone derivatives containing isoxazoline moiety have been synthesized. Generally, Chalcones are unsaturated ketones bearing (-CO-CH=CH-) as reactive ketoethylenic group that give the bright yellow colored compounds due to this chromophore group.  Firstly, chalcones (IIa-d) have been prepared by cyclocondensation (Claisen-Schmidt condensation) of triphenyl aminobenzaldehyde with different substituted acetophenone in ethyl alcohol to produce a series of chalcones compounds with bright yellow colored as a

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Publication Date
Fri Jun 28 2024
Journal Name
Al-rafidain Journal Of Medical Sciences ( Issn 2789-3219 )
Synthesis, Characterization, Molecular Docking, ADMET Study, and Antimicrobial Evaluation of New Mannich Bases of Isatin–Thiazole Imine Bases
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Background: The isatin molecule is present in many natural substances, including plants and animals, and is used to prepare compounds with various biological activities. Objectives: To synthesize a new series of isatin derivatives with the expectation that they will have antimicrobial activity. Methods: Thiazole Schiff bases were synthesized from various Mannich bases of isatin to evaluate their antimicrobial properties. Initially, Mannich bases (2a–e) were synthesized by reacting isatin with formaldehyde and different secondary amines. Subsequently, they were treated with 2-aminothiazole to yield the final compounds (3a–e). Spectroscopic characterization was done via FT-IR and 1H-NMR. The antimicrobial screening was conducted o

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Publication Date
Tue Mar 15 2016
Journal Name
International Journal Of Pharmacy And Pharmaceutical Sciences
SYNTHESIS, CHARACTERIZATION AND PRELIMINARY ANTIMICROBIAL EVALUATION OF NEW SCHIFF BASES OF AMPICILLIN AND AMOXICILLIN DERIVED FROM ISATIN DERIVATIVES
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Objectives: Six different Schiff bases were synthesized from ampicillin and amoxicillin with isatin, 5-bromoisatin, and 5-nitroisatin. Methods: Ampicillin and Amoxicillin are linked directly through their α-amino groups to the acyl side chain with isatin and isatin derivatives by nucleophilic addition using glacial acetic acid as a catalyst. Results: chemical structures of these Schiff bases were confirmed using FTIR, 1H NMR and elemental microanalysis. The antibacterial activity was evaluated by measuring minimum inhibitory concentration (MIC) values and showed various degrees of antibacterial activities when compared with parent drugs. Compounds 1a and 2b, which are the Schiff bases of ampicillin and amoxicillin with isatin, showed very

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Publication Date
Sun Jun 05 2022
Journal Name
Egyptian Journal Of Chemistry
Synthesis, Characterization, and Biological Activity of New Metal Ions Complexes with Schiff Base Derived from 2-Acetylthiophene and Isatin-3-Hydrazone
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This study describes the preparation of a new bidentate Schiff base derived from the condensation of Isatin-3-hydrazone with 2-acetylthiophene and the preparation of new series of complexes with a good yield. The prepared ligand was characterized by IR, UV-Vis, C.H.N.S elemental analysis, 1H and 13C NMR, LC-Mass spectroscopy, and physical measurements. Its complexes were analyzed by C.H.N.S elemental analyses, UV-Vis., FTIR, NMR, LC-Mass Spectra, atomic absorption spectroscopy, magnetic susceptibility, and conductivity measurements The results from spectroscopy and measurement studies showed that the ligand coordinated to the metal ion as a bidentate ligand via oxygen and nitrogen, forming an octahedral geometry around it. In vitro antimicr

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Publication Date
Sat Jan 20 2024
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Synthesis, Biological and Medicinal Evaluation of New Boric Acid Ester Derived From Antibiotic Drug with Some of Its Metal Complexes
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Synthesis of new ligand, namely [bis(2-(2-methyl-5-nitro-1H-imidazol-1-yl)ethyl) hydrogen borate] (BIB), utilizing the reaction of metronidazole with boric acid in mole ratio (2:1), as well as the metal complexes with [Ni(II) and Cu(II)], were synthesized. All synthesized compounds were characterized by utilizing spectroscopic techniques such as FTIR, 1H-NMR, thermal analysis (T.G., UV-Vis), and atomic absorption (A.A.S.), as well as micro elemental analysis (C.H.N.), melting point (m.p), magnetic susceptibility, molar conductivity, and chloride content measurements. All complexes were paramagnetic, and the electrolyte and the suggested geometries were tetrahedral for nickel and octahedral for copper. In addition, all the transition meta

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Publication Date
Sun Apr 30 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Synthesis and Study Biological Activity of Some New Isoxazoline and Pyrazoline derivatives
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   This work involves synthesis of novel Schiff bases derivatives contining isoxazoline or pyrazoline units starting with chalcons . 4-Aminoacetophenone was reacted with 3-nitrobenzaldehyde in basic medium giving chalcone [I] by claisen-schemidt reaction. The chalcone [I]  was reacted with hydroxylamine hydrochloride giving isoxazoline [II]  in basic medium. The chalcone [I] could also react with hydrazitne hydrate to give pyrazoline [III]  . The novel Schiff bases with structural formula [IV] and [V] were prepared by the reaction of amino compounds ; isoxazoline [II] and pyrazolines [III] with p-substituted aldehydes or p-subsituted ketones, respectively in dry benzene using drops of glacial acetic acid as a cat

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Publication Date
Sat Jan 01 2022
Journal Name
Materials Today: Proceedings
Molecular Docking, Synthesis, characterization and preliminary cytotoxic evaluation of new 1, 3,4-Thiadiazole derivatives as EGFR inhibitors
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Publication Date
Wed Jun 20 2018
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis, Characterization and Antimicrobial Evaluation with DFT Study of New Two-Amino-4-(4-Chlorophenyl) Thiazole Derivatives
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2-amino-4-(4-chloro phenyl)-1,3-thiazole (1) was synthesized by refluxing thiourea with para-chloro phenacyl bromide in absolute methanol. The condensation of amine compound (1)  with phenylisothiocyanate in the presence of pyridine will  produce 1-(4-(4-chlorophenyl)thiazol-2-yl)-3-phenylthiourea(2), which is  upon treatment with 2,4 dinitrophenyl hydrazine by conventional method, afforded 1- ( 4 - ( 4 – chlorophenyl ) thiazol – 2 – yl ) – 3 - phenylhydrazonamide,N' - ( 2 , 4 -dinitrophenyl) ,(3).The characterization of the titled compounds were performed utilizing FTIR spectroscopy, 1HNMR and CHNS elemental analysis, and by me

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Publication Date
Sun May 10 2020
Journal Name
Baghdad Science Journal
Characterization and Biological Activity of Some New Derivatives Derived from Sulfamethoxazole Compound: new derivatives from sulfamethoxazole drug.
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 A new series of Sulfamethoxazole derivatives was prepared and examined for antifibrinolytic and antimicrobial activities. Sulfamethoxazole derivatives bear heterocyclic moieties such as 1,3,4-thiadiazine {3},  pyrazolidine-3,5-diol {4} 6-hydroxy-1,3,4-thiadiazinane-2-thione {5} and [(3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-4-yl)diazenyl] {8}. Their structures were elucidated by spectral methods (FT-IR, H1-NMR). Physical properties are also determined for all compound derivatives.  Recently prepared compounds were tested for their antimicrobial activity in the laboratory. Each screened compound showed good tendency to moderate antimicrobial activity.

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Publication Date
Sun Mar 07 2010
Journal Name
Baghdad Science Journal
Synthesis, Characterization and Antimicrobial activity Study Via some new Schiff bases for Trimethoprim
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This search reports the synthesis of some new series of Schiff base compounds for trimetheprim derivatives which known high been known as a medicinal effectiveness. Trimetheprim was condensed with several substituted aldehydes compounds.(4-dimethyl amine benzaldehyde , propanal , salicaldehyde, 2.4 dimethoxy benzaldehyde and 4- methyl benzaldehyde) to obtain Schiff base products(1a-5a) and several substituted ketones compound (4-aminoacetophenone,4-chloroacetophenone, isobutyleketone, acetylacetone and acetophenone) to obtain Schiff base products(6b-10b) in ethanol in the presence of concentrated sulphuric acid as a catalyst to yield the Schiff base. The structure of synthesized compounds has been established on the basis of their Chemical

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