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Synthesis, Characterization, and Antimicrobial Evaluation of New Ceftriaxone Derivatives

The present study was designed to synthesize a number of new Ceftriaxone derivatives by its involvement with a series of different amines, through the chemical derivatization of its 2-aminothiazolyl- group into an amide with chloroacetyl chloride, which on further conjugation with these selected amines will produce compounds with pharmacological effects that may extend the antimicrobial activity of the parent compound depending on the nature of these moieties.

Ceftriaxone was first equipped with a spacer arm (linker) by the action of chloroacetyl chloride in aqueous medium and then further reacted with seven different aliphatic and aromatic amines which resulted in the production of the aimed final target products. The syntheses have 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. All the final synthesized compounds were screened for their antimicrobial activity against selected microorganisms and showed excellent antibacterial and antifungal activities in comparison to Ceftriaxone, Cephalexin and Fluconazole.

The new Ceftriaxone derivatives have broadened the antimicrobial spectrum of the parent compound in having an extra antifungal activity in addition to its original antibacterial activity.

Keywords: Ceftriaxone, 2-aminothiazole, Antimicrobial activity, Antifungal activity, Ceftriaxone derivatives.

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Publication Date
Sun Sep 01 2013
Journal Name
Baghdad Science Journal
Synthesis and Characterization of New phenolic Schiff bases Derivatives Based on Terephthaladehyde

A variety of new phenolic Schiff bases derivatives have been synthesized starting from Terephthaladehyde compound, all proposed structures were supported by FTIR, 1H-NMR, 13C-NMR, Elemental analysis, some derivatives evaluated by Thermal analysis (TGA).

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Publication Date
Sun Dec 06 2015
Journal Name
Baghdad Science Journal
Synthesis and Characterization of Some New Benzodiazepinium Salt Derivatives under microwave Irradiation

An attempt to synthesize the benzoimidazol derivatives from the reaction of o-phenylenediamine and benzoic acid derivatives in the presence of ethanol and various ketones under microwave irradiation, 1 , 5 - benzodiazepinum salt derivatives were obtained instead of them. Unexpected reaction was happened for synthesis a new series of benzodiazepinium salt derivatives in a selective yield . The reaction mechanism was also discussed. The new compounds were purified and identified their structures were elucidated using various physical techniques like; FT- IR spectra, micro elemental analysis (C.H.N) and 1H NMR spectra.

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Publication Date
Thu Dec 01 2022
Journal Name
Journal Of Molecular Structure
A new thiazoldinone and triazole derivatives: Synthesis, characterization and liquid crystalline properties

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Publication Date
Thu Jun 30 2022
Journal Name
International Journal Of Drug Delivery Technology
Synthesis of New Substituted Coumarin Derivatives containing Schiff-Base as Potential Antimicrobial and Antioxidant Agents

By unusual method for separating two isomers of a substituted nitro-coumarin using a soxhlet extractor and in controlling temperature to get a selective nitration reaction, several new Schiff base coumarins were synthesized from nitro coumarins as starting material, which were reduced by Fe in glacial acetic acid to produce corresponding amino coumarin derivatives. Then the latter was reacted with different aromatic aldehydes to produce the desired Schiff bases derivatives. After characterization by Fourier transform infrared (FT-IR), Proton nuclear magnetic resonance (1HNMR) and Carbon-13 nuclear magnetic resonance (C-NMR), all these compounds were evaluated as potential Antimicrobial and Antioxidant Agents.

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Publication Date
Wed Jan 01 2003
Journal Name
Ibn Al-haitham . J . For Pure & Appl Sci
Synthesis and characterization of new orttho - amino phenyl thio derivatives and their complexes

Two ligand ortho-amino phenyl thio benzyl (L1) and 1,3 bis (ortho - amino phenyl thio ) acetone (L2) and their complexes have been prepared and characterized . The L1 ligand is lossing phenyl group on complexcation and forming 1,2 bis (ortho - amino phenyl thio ) ethane L3 and this tetrahedrally coordinated to the metal ion ( M+2 = Ni , Cu , Cd ) and octahedrally coordinated with mercury and cobalt ions , while the ligand L2 is behave as tridentate ligand forming octahedrally around chrome metal ion . Structural , diagnosis were established by i.r , Uv- visible , conductivity elemental analysis and (mass spectra , H nmr spectra for( L1 , L2 ) .

Publication Date
Sun Sep 04 2016
Journal Name
Baghdad Science Journal
Synthesis and Characterization of Some New Pyrazoline and Isoxazoline Derivatives as Antibacterial Agents

In this paper some chalcones (C1-C8) are prepared based on the reaction of one mole of substituted acetophenone with one mole of substituted benzaldehydes in the presence of (40%) sodium hydroxide as a base. Pyrazolines (P1–P8) are prepared from the reaction of chalcones (C1-C8) with hydrazine hydrate. Isoxazoline (I1-I8) is prepared from the reaction of chalcones (C1-C8) with hydroxyl amine hydrochloride in the presence of (10%) sodium hydroxide as a base. These compounds are characterized by using various physical and spectral methods. The compounds are screened for their in vitro antibacterial activity using gram-positive bacteria and gram-negative bacteria. Several derivatives of pyrazolines and isoxazolines are produced well to moder

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Publication Date
Tue Nov 01 2022
Journal Name
Chemical Methodologies
Synthesis and Characterization of New Substituted Coumarin Derivatives and Study Their Biological Activity

New substituted coumarins derivatives were synthesized by using nitration reaction to produce different nitro coumarin isomers which were separated from these isomers by using different solvent, and the reduction of nitro compounds was done to give corresponding amino coumarins. Temperature and reaction time of reaction were very important factors in determining the most productive nitro isotopes. A low temperature for three hours was sufficient to give a high product of a compound 6-nitro coumarin while increasing the temperature for a period of twenty-four hours that gave a high product of 8-nitro-coumarin. The synthesized compounds were confirmed by FT-IR,1 H-NMR, and13 C-NMR spectroscopy and all final compounds were tested for their ant

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Publication Date
Sat Jun 29 2024
Journal Name
Iraqi Journal Of Pharmaceutical Sciences( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis and Characterization of New 5-Fluoroisatin-Chalcone Conjugates with Expected Antimicrobial Activity

Pathogenic microorganisms are becoming more and more resistant to antimicrobial agents. So the synthesis of new antimicrobial agents is very important. In this work, new 5-fluoroisatin-chalcone conjugates 5(a–g) were synthesized based on previous research that showed the modifications of the isatin moiety led to the synthesis of many derivatives that have antimicrobial activity. 4-aminoacetophenone reacts with 5-fluoroisatin to form Schiff base (3), which in turn reacts with two different groups of aromatic (carbocyclic and heterocyclic) aldehydes 4(a–g) separately to form the final compounds 5(a–g). Proton-nuclear magnetic resonance (¹H-NMR) and Fourier-transform infrared (FT-IR) spectroscopy were used to confirm the chemic

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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 and Preliminary Biological Activity Evaluation of New N- Substituted Phthalimide Derivatives

A

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

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Publication Date
Mon Mar 15 2021
Journal Name
Egyptian Journal Of Chemistry
Synthesis and Characterization of some Tetrazole Derivatives and Evaluation of their Biological Activity

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