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bijps-1022
Synthesis and Preliminary Biological Activity Evaluation of New N- Substituted Phthalimide Derivatives
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A new series of bases of Schiff (H2-H4) derived from phthalic anhydrideweresynthesized. These Schiff bases were prepared by the reaction of different amines (tyrosine methyl ester, phenylalanine methyl ester, and isoniazid) with the phthalimide derived aldehyde with the aid of glacial acetic acid or triethylamine ascatalysts. All the synthesized compounds were characterized by (FT-IR and 1HNMR) analyses and were in vitro evaluated for their antimicrobial activity against six various kinds of microorganisms. All the synthesized compounds had been screened for their antimicrobial activity against two Gram-positive bacteria “Staph. Aureus, and Bacillus subtilis”, two Gram-negative bacteria “Escherichia coli, and Klebsiella pneumoniae”, and two fungi species “Candida tropicalis and Candida albicans” using concentrations of 62.5, 125 and 250 µg\mLof derivative in dimethyl sulfoxide(DMSO). All the synthesized compounds showed no activity at all against Gram-positive bacteria, for Gram-negative bacteria and fungi they showed moderate or no activity except compound H1revealedhigh antifungal activityagainstCandida tropicalisat concentrations 125 and 250 µg\ mL.

Keywords: Schiff base, phthalic anhydride, antimicrobial.

 

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Publication Date
Wed Jun 26 2019
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis, Characterization and Preliminary Study of the Anti-Inflammatory Activity of New Pyrazoline Containing Ibuprofen Derivatives
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Publication Date
Thu Jun 25 2020
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis, Characterization and Antibacterial Activity Evaluation of New Indole-Based Derivatives
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A new series of N-acyl hydrazones (4a-g) derived from indole-3-propionic acid (IPA) were synthesized. These N-acyl hydrazones were prepared by the reaction of 3-(1H-indol-3-yl) propane hydrazide and aldehyde in the existence of glacial acetic acid as a catalyst. 1HNMR and FT-IR analyses were used to identify the synthesized compounds and they were in vitro evaluated as antibacterial agents against six different types of microorganisms by using well diffusion method. All the tested N-acyl hydrazones (4a-g) displayed moderate activity against the Gram-negative E.coli, comparable to that of Amoxicillin. Some of the tested N-acyl hydrazones also exhibited intermediate activity ag

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Publication Date
Thu Apr 29 2021
Journal Name
Iraqi Journal Of Science
Synthesis and Identification of Some New Derivatives of ([Benzyl Thio) Benzimidazole -N- (Methylene-5-Yl)] - 4,5- Di Substituted 1,2,4-Triazole and Evaluation of Their Activity as Antimicrobial and Anti-Inflammatory Agents
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New 2-Mercaptobenzimidazole derivatives were synthesized. 4,5-disubsitituted 1,2,4-Triazole compounds 1b-2c were synthesized from 2-(benzylthio) benzimidazole compound a, which was then reacted with (NaH) in dioxane at a temperature of (0-5 C°) to produce the salt of compound a. Then the salt was reacted with ethyl chloro acetate to yield Ethyl 2-(benzylthio) benzimidazole acetate compound b. Compound b was converted to triazole derivatives by two pathways. The first pathway was reacting compound b with semicarbazide, thiosemicarbazide and phenylsemicarbazide in DMSO as a solvent to gain compounds 1b-3b, which were then

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Publication Date
Mon Mar 01 2010
Journal Name
Journal Of Kerbala University
Synthesis And Biological Activity Of Some New Compounds Containing 1,2,4-Triazole And Their Derivatives
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Condensation of 1,2- dibromo ethane with para hydroxy benzoic acid gave 1,2-Ethane-bis- 4-oxybenzoic [1]. This Compound was converted with the thionyl chloride to give 1,2-Ethane-bis- 4-oxybenzoyl chloride [2]. Reaction of compound [2] with thiosemicarbizades gave 1,2-Ethanebis[4-oxybenzoyl-thiosemicarbazide] [3] and opteined 1,2-Ethane-bis[3-mercapto-5-phenoxy- 1,2,4-triazole] [4] from treatment compound [3] with NaOH (4%) .The new compounds 1,2- Ethane-bis[3-(substituted thioacyl)-4-(substituted acyl)-5 phenoxy-1,2,4-triazole] [5a-d] and 1,2- Ethane-bis[3-(substituted alkylthio)-5 phenoxy-1,2,4-trizole] [5e-f] derived from compound [4] were synthesized and characterized by physical and spectral data. All the compounds [4], [5a-d] and [5e-

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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 Feb 08 2023
Journal Name
Iraqi Journal Of Science
Synthesis, Identification and Evaluation Biological Activity for Some New Triazole, Triazoline and Tetrazoline Derivatives From 2-Mercapto-3-phenyl-4(3H)Quinazolinone
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This research, involved synthesis of some new 1,2,3-triazoline and 1,2,3,4-tetrazole derivatives from antharanilic acid as starting material .The first step includes formation of 2-Mercapto-3-phenyl-4(3H)Quinazolinone (0) through reacted of anthranilic acid with phenylisothiocyanate in ethanol, then compound (0) reaction with chloro acetyl chloride in dimethyl foramamide (DMF) to prepare intermediate S-(α-chloroaceto-2-yl)-3-phenylquinazolin-4(3H)-one (1); compound (1) reacted with sodium azide to yield S-(α-azidoaceto-2-yl)-3-phenylquinazolin-4(3H)-one (2), while Schiff bases (3-10) were prepared from condensation of substituted primary aromatic amines with different aromatic aldehydes in absolute ethanol as a solvent. Compound (2) re

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Publication Date
Mon Feb 08 2016
Journal Name
Iraqi Journal Of Science,
Synthesis, Identification and Evaluation Biological Activity for Some New Triazole, Triazoline and Tetrazoline Derivatives From 2-Mercapto-3- phenyl-4(3H)Quinazolinone
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This research, involved synthesis of some new 1,2,3-triazoline and 1,2,3,4- tetrazole derivatives from antharanilic acid as starting material .The first step includes formation of 2-Mercapto-3-phenyl-4(3H)Quinazolinone (0) through reacted of anthranilic acid with phenylisothiocyanate in ethanol, then compound (0) reaction with chloro acetyl chloride in dimethyl foramamide (DMF) to prepare intermediate S-(α-chloroaceto-2-yl)-3-phenylquinazolin-4(3H)-one (1); compound (1) reacted with sodium azide to yield S-(α-azidoaceto-2-yl)-3-phenylquinazolin-4(3H)-one (2), while Schiff bases (3-10) were prepared from condensation of substituted primary aromatic amines with different aromatic aldehydes in absolute ethanol as a solvent. Compound (2)

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Publication Date
Mon May 15 2023
Journal Name
Iraqi Journal Of Science
Synthesis and Characterization of Some New Nucleoside Analogues from Substituted Benzimidazole and Evaluation of Their Biological Activities
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This research includes the synthesis of some new nucleoside analogues via 1,3-
dipolar cycloadditon reaction starting with 1,3,4,6- Tetra- O-benzoyl –2 – azido-2-
deoxy- β – D- fructofuranose (F3) which was prepared in three steps ,protection
(benzoylation ) , bromination and azotation ((F1-F3) from D- fructose as sugar
moiety while the base moiety , 2-substituted benzimidaole derivatives (A1-A5)
were synthesized by condensation of O-phenylenediamine with different aromatic
aldehyde .
Nucleophilic substitution of propargyl bromide with benzimidaole derivatives (gave
the N- substituted compounds (B1-B5) which were reacted with azido sugar through
1,3- dipolar cycloadditon reaction to give nucleoside analo

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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 Apr 23 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Synthesis and Characterization of New Schiff Bases Derived from Reaction of The Cefixime with Benzaldehyde Derivatives and Evaluation of Their Biological Activity
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  The Schiff bases (1-10) were synthesized by the reaction of cefixime  with aldehydes derivatives. The characterization of Schiff bases were carried out, by using   spectroscopic techniques including IR, U.V – Vis, H1-NMR, EI-MS along with elemental analyses (C.H.N.).

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