Der Pharma Chemica
Journal for Medicinal Chemistry, Pharmaceutical Chemistry and Computational Chemistry

Abstract

Synthesis, Characterization and Preliminary Antimicrobial Evaluation of New Derivatives of Ceftazidime

Author(s): Shakir M Alwan, Mohammed H Mohammed, Alaa A Alhassan

Cephalosporins derivatives remain as one of the most versatile class of compounds against bacteria and therefore, are useful for further molecular exploration. The development of new derivatives of ceftazidime with improved activity against resistant microbes is of high potential. Chemical synthesis of four new derivatives of ceftazidime, in which amino acids was linked to ceftazidime by substitution of pyridine ring at C3 position gave the target derivatives A (1-4) as a first line. In addition, to the N-acylation of the free amine group of aminothiazole ring by acids chloride to obtain three target derivatives B (1-3) as a second line. New ceftazidime derivatives were successfully prepared, characterized and identified using; melting point, TLC, spectral (FT-IR) and elemental microanalysis (CHNS). All target compounds A (1-4) and B (1-3) were evaluated for their antibacterial activity against certain bacteria such as; Escherichia coli and Pseudomonas aeruginosa, Streptococcus pneumoniae and Staphylococcus aurous. Generally, all seven new derivatives of ceftazidime showed significant antibacterial activity against the tested microorganisms, especially G (-) bacteria as compared to ceftazidime.


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