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bijps-392
Synthesis, Characterization, and Antimicrobial Evaluation of New Ceftriaxone Derivatives
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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
Tue Jun 20 2023
Journal Name
Baghdad Science Journal
Preparation, characterization, antioxidant activity of 1-(2-furoyl) thiourea derivatives and study the molecular docking of them as potent inhibitors of Urease enzyme
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In this work, we synthesized thirteen compounds of 1-(2-furoyl)thiourea derivatives 1-13 by conversion of 2-furoyl chloride to 2-furoyl isothiocyanate by reacting it with potassium thiocyanate in dry acetone in a quite short reflux time then, in the same pot, different of (primary and secondary amines) were added individually to achieve thiourea derivatives. The products were characterized spectroscopically using (FT-IR, 1H NMR and 13C NMR) techniques. Some of them were evaluated as antioxidant agents using DPPH radical scavenging method, and all were examined theoretically as enzyme inhibitors against Bacillus pasteurii urease (pdb id: 4ubp) and  by studying  molecular docking using Autodock (4.2.6) software.

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Publication Date
Wed Jun 30 2021
Journal Name
Iraqi Journal Of Market Research And Consumer Protection
SYNTHESIS, CHARACTERIZATION, AND STUDY THE BIOLOGICAL ACTIVITY OF SOME SCHIFF'S BASES, AND 1,3 - OXAZEPINE COMPOUNDS DERIVED FROM SULFAMETHOXAZOLE DRUG: SYNTHESIS, CHARACTERIZATION, AND STUDY THE BIOLOGICAL ACTIVITY OF SOME SCHIFF'S BASES, AND 1,3 - OXAZEPINE COMPOUNDS DERIVED FROM SULFAMETHOXAZOLE DRUG
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This study including synthesis of some new Schiff bases compounds [1‐6] from the reaction of Sulfamethoxazole drug with some aromatic aldehydes in classical Schiff base method then treatment Schiff  bases with succinic anhydride to get oxazepines rings [7-11]These derivatives were characterized by melting point, FT‐IR, 1H NMR and mass spectra. Some of synthesized compounds were evaluated in vitro for their antibacterial activities against three kinds of pathogenic strains Staphylococcus aureus, Escherichia coli

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Publication Date
Tue Mar 28 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Preparation, Characterization, and in - vivo Evaluation of Daptomycin Poly(D,L-lactide-co-glycolide) Microspheres
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             Polymeric microsphere devices occupy a wide range in the field of controlled drug delivery. Subcutaneous injectable preparations of Poly(Lactide-co-Glycolide) (PLGA) microsphere of Daptomycine were prepared by solvent extraction/evaporation technique using different copolymers ratio and molecular weights. Four formulations were prepared (F1-F4) and characterized in term of particle size, surface morphology, bulk density and porosity in addition to the drug content. The effects of the above parameters on the in-vitro release study were evaluated. These formulas were evaluated also for their in-vivo release profile using rat (as an animal model) and

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Publication Date
Sun Dec 01 2013
Journal Name
Journal Of International Academic Research For Multidisciplinary
SYNTHESIS AND LIQUID CRYSTALLINE BEHAVIOUR OF NEW SERIES CONTAINING 1, 3-OXAZEPINE AND 1, 3-THIAZOLE RINGS
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The synthesis and properties of two new series of compounds having 1,3-Oxazepineand 1,3-thiazole rings connected through azo linkage are reported. These compounds weresynthesized by the reaction of phthalic anhydride with Schiff bases. The molecular structuresof these compounds were verified by elemental analysis, FTIR and 1HNMR spectroscopy.The mesomorphic behaviors of these compounds were studied by optical polarizedmicroscopy (OPM) and differential scanning calorimetry (DSC). All compounds of the twoseries show liquid crystalline properties. The influence of the central oxazepine and thiazolerings and the terminal substituents on the type and temperature range of the mesomorphousproperties of these compounds has been elucidated

Publication Date
Sun Dec 01 2019
Journal Name
Journal Of Medicinal And Chemical Sciences
Synthesis and Identification of New 2-Substituted-1,3,4-Oxadiazole Compounds from Creatinine and Study Their Antioxidant Activities
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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 and Preliminary Pharmacological Study of Sulfonamide Conjugates with Ibuprofen and Indomethacin as New Anti-Inflammatory Agents
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          4-aminobenzenesulfonamide conjugates of ibuprofen (compound 10) and indomethacin (compound 11) have been designed and synthesized by the reaction of sulfanilamide (compound 7) with 2-(4-isobutylphenyl) propanoic acid (ibuprofen) and 2-(1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1H-indol-3-yl)acetic acid (indomethacin) for the evaluation as potential anti-inflammatory agents with expected selectivity against COX-2 enzyme. In vivo acute anti-inflammatory activity of the synthesized final compounds (10 and 11) was evaluated in rats using egg-white induced edema model of inflammation in a dose equivalent to (10mg/Kg) of ibuprofen and (2mg/kg) of indomethacin. The tested compounds pr

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Publication Date
Mon Jul 20 2026
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Synthesis and Antibacterial Activity of New Hybrid Molecules Containing 1,3,4-Thiadiazole and 1,3,4-Oxadiazole Bearing Ibuprofen Moiety
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A series of novel hybrid molecules containing 1,3,4-oxadiazole and 1,3,4-thiadiazole moieties bearing an ibuprofen moiety were designed, synthesized, and evaluated for their in vitro antibacterial activity against Gram-positive and Gram-negative bacteria. A carboxylic acid compound with a 1,3,4-thiadiazole unit was synthesized via the coupling reaction of 5-(1-(4-isobutylphenyl) ethyl)-1,3,4-thiadiazol-2-amine with benzoic acid. This compound was then used as the starting material to make several new 1,3,4-oxadiazole derivatives through ring closure reactions, after first converting it to its ester (methyl 4-(5-(1-(4-isobutylphenyl)ethyl)-1,3,4-thiadiazol-2-yl) benzoate) and then to the acid hydrazide (4-(5-(1-(4-isobutylphenyl) eth

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Publication Date
Wed Jan 01 2025
Journal Name
Ieee Access
Design and Comprehensive Study of a New Soft Electromagnetic Actuator: Mathematical Modeling, Numerical Analysis, and Experimental Evaluation
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Soft robotics offers a flexible alternative to rigid systems, enabling safe and adaptive interaction in biomedical, wearable, and unstructured environments. Among available actuation methods, soft electromagnetic actuators are notable for their fast response, low operating voltage, and ease of integration. However, some designs require pre-stretching mechanism, which produces an external force to maintain the separation between the coil and permanent magnets. Additionally, there is a mechanical complexity and difficulty in calibrating the spring parameters precisely. Furthermore, the pre-stretching mechanism increases the electromagnetic force required to counteract the opposing spring force, leading to a significant increase in power consu

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Publication Date
Wed Mar 05 2025
Journal Name
Bulletin Of The Chemical Society Of Ethiopia
Synthesizing, characterization of some metal ion complexes with new azo dye and studying antioxidant and anticancer (MCF-7)
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This new azo dye 7-(3-hydroxy-phenylazo)-quinoline-8-ol was subsequently used to prepare a series of complexes with the chlorides of Fe, Co, Zn, Ru, Rh and Cd. The compounds identified by 1H and 13C-NMR, FT-IR, UV-Vis, mass spectroscopy, as well as TGA, DSC, and C.H.N., conductivity, magnetic susceptibility, metal and chlorine content. The results showed that the ligand behaves in a trigonal behavior, and that the complexes gave tetrahedral, except for Fe, Ru and Rh octahedral was given, that all of them are non-electrolytes. The effectiveness of both the compounds in inhibiting free radicals was evaluated by the ability to act as an antioxidant was measured using DPPH as a free radical and gallic acid as a standard substance, the

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Publication Date
Sat Jun 01 2024
Journal Name
Results In Engineering
Electrochemical preparation and characterization of a new configuration SnO2 anode and its application for treating petroleum refinery wastewater
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