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bijps-401
Synthesis and Antimicrobial Evaluation of New 6 and7 Substituted Derivatives of Coumarin
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A series of benzohydrazide derivatives attached to coumarin moiety at position 6 and 7 have been synthesized. The reaction of coumarin derivatives (coumarin I and II) with p-nitrophenyl hydrazine yield Schiff bases (compound1a and IIa).These Schiff bases were refluxed with benzoyl chloride to give benzohydrazide derivatives of coumarin substituted at its 6 or 7 nucleus position (Ia1 and IIa1).The reaction and the purity of the products were checked by thin layer chromatography (TLC). The structures of the final compounds  and  their intermediates were confirmed by their melting points, infra red spectroscopy, and elemental microanalysis(CHN).

Compounds (Ia1 and IIa1) were evaluated for  their preliminary antibacterial and antifungal activities. Compound (IIa1) has good antibacterial activity against Staphylococcus aureus   other  than bacterial species, and was equivalent to ofloxacin as (standard drug).

Key word: Coumarin, Schiff base, benzohydrazide derivatives, antimicrobial activity.

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Publication Date
Sun Mar 03 2013
Journal Name
Journal Of Al-nahrain University
Synthesis and Characterization of Some New 1,2,3-Triazole, Pyrazolin-5-one and thiazolidinone Derivatives
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Five membered heterocyclics derivatives were synthesized in this work by three routes. The first route includes the synthesis of N-benzoic acid 1,2,3,-triazole derivatives (3),(4) by diazotation of methyl-2-amino benzoate and treating the resulted salt (1) with sodium azide and ethyl acetoacetate or acetyl acetone, respectively. In the second route, derivatives of pyrazole (8) pyrazolin-5-one (9), (10) were prepared by the reaction of the salt (1) with some active methylene compounds to give the corresponding hydrazones derivatives (5-7) which then they were treated with hydrazine hydrate. The third route afforded the synthesis of three derivatives (12), (15a), (15b) of thiazolidinone by two different methods. AII compounds were confirmed b

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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
Thu Mar 30 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis of New Cyclic Amines-Linked Metronidazole Derivatives as Possible Prodrugs
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         Certain cyclic amine derivatives of metronidazole via acetate spacer were prepared. Cyclic amines used are piperidine and piperazine to improve the physicochemical properties and reduce some of metronidazole side effects. This is believed to be done by modification of its structural features to get prodrugs with improved properties over that of metronidazole. The present work includes esterification of metronidazole with choroacetic acid, N-alkylation of the cyclic amines by the halogenated ester and characterization of their structures by spectral(UV and IR) and elemental(CHN)analysis.The melting points, degree of solubilities and partition coefficients were also determined. Both metronid

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Publication Date
Sun Dec 25 2022
Journal Name
International Journal Of Drug Delivery Technology
Synthesis, Characterization of New Isatin-Ibuprofen Derivatives with Expected Biological Activity
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Ibuprofen is one of the most important members of NSAIDs, named aryl propionic acid derivative. Isatin (1H-indole-2,3-dione) is an important molecule of heterocyclic compounds that have many biological activities. This work illustrates the synthesis of new ibuprofen-isatin derivatives by connecting ibuprofen hydrazide with different isatin derivatives by a condensation reaction, followed by characterization by fourier-transform infrared spectroscopy (FTIR) and proton nuclear magnetic resonance (1H-NMR) spectroscopy. The anti-inflammatory activity was evaluated by using the egg-white induce edema method for all the synthesized compounds (5-8), the compounds 5 and 6 showed better anti-inflammatory activity than ibuprofen as a standard compoun

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Publication Date
Sun Dec 25 2022
Journal Name
International Journal Of Drug Delivery Technology
Synthesis, Characterization of New Isatin-Ibuprofen Derivatives with Expected Biological Activity
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Ibuprofen is one of the most important members of NSAIDs, named aryl propionic acid derivative. Isatin (1H-indole-2,3-dione) is an important molecule of heterocyclic compounds that have many biological activities. This work illustrates the synthesis of new ibuprofen-isatin derivatives by connecting ibuprofen hydrazide with different isatin derivatives by a condensation reaction, followed by characterization by fourier-transform infrared spectroscopy (FTIR) and proton nuclear magnetic resonance (1H-NMR) spectroscopy. The anti-inflammatory activity was evaluated by using the egg-white induce edema method for all the synthesized compounds (5-8), the compounds 5 and 6 showed better anti-inflammatory activity than ibuprofen as a standard

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Publication Date
Sun Jun 05 2016
Journal Name
Baghdad Science Journal
Synthesis and Biological Effectiveness of Some new Azo Compounds as Derivatives of Nitrogen Bases
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In this study the new azo compounds (3compounds) for nitrogen bases (Adenine and Cytosine) are synthesized through two reaction steps (formation of diazonium salt and coupling reaction). The compounds have been characterized by FTIR, melting point, and ultra-violate (UV) spectra. All synthesized compounds have been estimated in vitro for their antimicrobial activities against two species of bacteria(E.coli, S.aureus)and one kind of fungi ( Aspergillus flavus) .The results show that these compounds have very good antibacterial and antifungal activities especially compounds 1 and 3.To study the effect of these compounds were making some physiological tests on rats are made ,the results of hematological study showed decreasing level of

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Publication Date
Thu Feb 01 2018
Journal Name
Iosr Journal Of Pharmacy And Biological Sciences
Synthesis, Characterization of Organic Derivatives Containing Heterocyclic Rings and Evaluation Their Antibacterial Activity
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Schiff bases (Sh1-Sh3) have been synthesized (p-aminophenol) was condensed with different aromatic aldehyde in ethanol inthe presence of glacial acetic acid as catalyst. These Schiff bases on treatment with monochloroacetyl choride gave 3-chloro-1-(4-hydroxyphenyl)-4-(substituted)azetidin-2-one(Az4-Az6), with αmercaptoacetic acid gave 3-(4-hydroxyphenyl)-2-( substituted)thiazolidin-4-one (Th7-Th9) and with anthranilic acid gave 3-(4-hydroxyphenyl)-2(substituted)-2,3-dihydroquinazolin-4(1H)-one (Qu10-Qu12). The purity of the derivatives was confirmed by TLC. The some compoundsidentify by (FT-IR and1H, 13C-NMR) data. Some of derivatives were evaluated activity against several microbesto determine ability to inhibit bacterial in some h

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Publication Date
Thu Jun 01 2023
Journal Name
Baghdad Science Journal
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-naphthaldehy

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Publication Date
Fri Apr 01 2022
Journal Name
Chemical Methodologies
Design, Synthesis of Imidazolone and Oxazepine Derivatives Bearing Imidazo (2, 1-b) Thiazole along with its Antimicrobial Activity
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A new methodology was applied to the synthesis of new imidazolones and oxyazepine derivatives containing imidazo thiazole fused rings. Starting with 5-(4-bromo phenyl) imidazo (2, 1-b) thiazole, which was synthesized using the standard procedure, the Carbaldehyed group was introduced at position 6 of 5-(4-bromo phenyl) imidazo (2, 1-b) thiazole. Then, this 6-carbaldehyed derivative was condensed with different substituted aromatic amines to afford new Schiff bases. The latter were cyclized into new oxazepine and imidazolone derivatives by using phthalic anhydride and glycine, respectively. These new derivatives were characterized by using FT-IR, 1HHNMR, and 13CNMR spectra, as well as examined (evaluated) for anti-bacterial and anti-fungal a

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Publication Date
Thu Jun 27 2019
Journal Name
Molecular Crystals And Liquid Cryst
A New Series of Triazine-core Based Mesogenic Derivatives: Synthesis, Characterization and Mesomorphic Study
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The synthesis, characterization and mesomorphic properties of two new series of triazine-core based liquid crystals have been investigated. The amino triazine derivatives were characterized by elemental analysis, Fourier transforms infrared (FTIR), 1HNMR and mass spectroscopy. The liquid crystalline properties of these compounds were examined by differential scanning calorimetry (DSC) and polarizing optical microscopy (POM). DSC and POM confirmed nematic (N) and columnar mesophase textures of the materials. The formation of mesomorphic properties was found to be dependent on the number of methylene unit in alkoxy side chains.

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