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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
Sat Jun 01 2024
Journal Name
Russian Journal Of Bioorganic Chemistry
Synthesis and Study the Biological Activity of Some New Pyrazole Compounds Containing 1,3,4-Oxadiazole Unite Through Vilsmeier–Haack Reaction
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Publication Date
Mon Mar 01 2021
Journal Name
Journal Of Physics: Conference Series
Synthesis and study the liquid crystalline properties of new compounds containing 5-methyl-2,4-dihydro-3H-pyrazol-3-one
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Abstract<p>The new compounds of pyrazolines were synthesized from the reaction of different acid hydrazide with ethylacetoacetate and ethanol under reflux. These compounds were obtained from many sequence reactions. The 4-acetyl-5-methyl-2,4-dihydro-3H-pyrazol-3-one compounds synthesized from the reaction of 5-methyl-2,4-dihydro-3H-pyrazol-3-one with acetyl chloride in calcium hydroxide and 1,4-dioxane. Finaly, Schiff bases were prepared via condensation reaction of products of mono- and tri ketone derivatives[IV]<sub>a, b</sub> with phenyl hydrazines as presented in (Scheme 1, 2). The synthesized compounds were identification by using FTIR, NMR and Mass spectroscopy (of some of them).</p> ... Show More
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Publication Date
Sun Jun 04 2017
Journal Name
Baghdad Science Journal
Synthesis, Characterization and Biological Activity of Schiff Bases Chelates with Mn(II),Co(II),Ni (II),Cu(II) and Hg(II)
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In this paper, some series of new complexes of Mn(II), Co(II), Ni (II) Cu(II) and Hg(II) are prepared from the Schiff bases (L1,L2). (L1) derived from 4-aminoantipyrine and O-phenylene dia mine then (L2) derived from (L1) and 2-benzoyl benzoic acid. Structural features are obtained from their elemental microanalyses, molar conductance, IR, UV–Vis, 1H, 13CNMR spectra and magnetic susceptibility. The magnetic susceptibility and UV–Vis, IR spectral data of the ligand (L1) complexes get square–planar and tetrahedral geometries and the complexes oflig and (L2) get an octahedral geometry. Antimicrobial examinations show good results in the sharing complexes.

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Publication Date
Sun Jun 04 2017
Journal Name
Baghdad Science Journal
Synthesis, Characterization and Biological Activity of Schiff Bases Chelates with Mn(II),Co(II),Ni (II),Cu(II) and Hg(II)
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In this paper, some series of new complexes of Mn(II), Co(II), Ni (II) Cu(II) and Hg(II) are prepared from the Schiff bases (L1,L2). (L1) derived from 4-aminoantipyrine and O-phenylene dia mine then (L2) derived from (L1) and 2-benzoyl benzoic acid. Structural features are obtained from their elemental microanalyses, molar conductance, IR, UV–Vis, 1H, 13CNMR spectra and magnetic susceptibility. The magnetic susceptibility and UV–Vis, IR spectral data of the ligand (L1) complexes get square–planar and tetrahedral geometries and the complexes oflig and (L2) get an octahedral geometry. Antimicrobial examinations show good results in the sharing complexes.

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Publication Date
Wed Jun 30 2021
Journal Name
Iraqi Journal Of Market Research And Consumer Protection
RATE CONSTANT OF SOME AMINO DERIVATIVES DISSOCIATION: RATE CONSTANT OF SOME AMINO DERIVATIVES DISSOCIATION
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Amino glycoside derivation including, Neomycin, Streptomycin, Kanamycin and Gentamycin with special reagents, which  are  benzoylchloride; benzene sulfonyl chloride and phthalic anhydride were made to enhance Uv-detectability for HPLC analysis. But there are many problems facing pre column derivation and in order to solve this, the conductivity of antibiotic derivatives were used to calculate the dissociation constant and the hydrolysis rate which determined concern type reaction. In addition the  characteristics those controlling the hydrolysis of antibiotic-derivatives were investigated.

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Publication Date
Mon Mar 27 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis of New B-adrenoceptor Blocking Agent Including 1,3,4 Thiadiazole with Expected Adrenoceptor Blocking Activity
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β-Adrenergic blocking agents, mostly comprising of β-amino alcohols, are of pharmaceutical significance and have received major attention due to their utility in the management of cardiovascular disorders including hypertension, angina pectoris, cardiac arrhythmias and other disorders related to the sympathetic nervous system. Most compounds available for clinical use belong to the aryloxypropanolamine series, which is considered the second generation of β-blocking agents. The present study includes the synthesis of compounds with an N-substituted oxypropanolamine moiety attached to the 1, 3, 4-thiadiazole derivatives. According to this information, eight compounds were synthesized and characterized by IR spectra and elemental m

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Publication Date
Sun Oct 01 2023
Journal Name
Baghdad Science Journal
Synthesis and Characterization of Co-Polymer (Styrene / Allyl 2,3,4,6-tetra-O-acetyl-β-D-glucopyranoside) and Studying some of its thermal properties
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In this research, a Co-polymer (Styrene / Allyl-2.3.4.6-tetra-O-acetyl-β-D-glucopyranoside) was synthesized from glucose in four steps using Addition Polymerization according to the radical mechanism using Benzoyl Peroxide (BP) as initiator. Initially, Allyl-2.3.4.6-tetra-O-acetyl-β-D-glucopyranoside monomer was prepared in three steps and the reaction was followed by (HPLC, FT-IR, TLC), in the fourth step the monomer was polymerized with Styrene and the structure was determined by FT-IR and NMR spectroscopy. The reaction conditions (temperature, reaction time, material ratios) were also studied to obtain the highest yield, the relative, specific and reduced viscosity of the prepared polymer was determined, from which the viscosity ave

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Publication Date
Sat Mar 31 2007
Journal Name
Um-salama Science Journal
Synthesis and Characterization of the Heavy Metals; Au(III), Pd(II), Pt(IV) and Rh(III) Complexes of S-Propynyl 2-Thiobenzimidazole
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Complexes of Au (III), Pd (II), Pt (IV ) and Rh(III) with S–propynyle-2- thiobenzimidazole (BENZA) have been prepared and characterized by IR and UV- Visible spectral methods in addition to magnetic and conductivity measurements and micro–elemental analysis (CHN).The probable structures of the new complexes have been suggested.

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Publication Date
Sun Jan 01 2023
Journal Name
Materials Today: Proceedings
Preparation, characterization and preliminary cytotoxic evaluation of 6-mercaptopurine-coated biotinylated carbon dots nanoparticles as a drug delivery system
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Publication Date
Sun Jan 01 2023
Journal Name
Materials Today: Proceedings
Preparation, characterization and preliminary cytotoxic evaluation of 6-mercaptopurine-coated biotinylated carbon dots nanoparticles as a drug delivery system
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