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Antibacterial Activities Of An Antibiotic On Complexation With Metals

By: Abid Riaz Ahmed | Dr. Muhammad Sabir.
Contributor(s): Dr. Khushi Muhammad | Mr. Razzaq Ali.
Material type: materialTypeLabelBookPublisher: 1997Subject(s): Department of Pharmaoclogy & ToxicologyDDC classification: 0544,T Dissertation note: The work presented in this thesis concerns the role of metal ions through chelation in drug design. The area received much attention since the claim that the complexes of drug substances with metal ions are more active and less toxic than the parent drug. In this work complexes of cephalexin with copper and zinc ions were prepared and characterized by microanalysis, IR and UV-vis spectrophotometry, magnetic measurement techniques, differential scanning calorimetry, and atomic absorption spectrometry. The complexes were found to be of ML2 type where M is the metal ion and L stands for the ligand. Both the complexes were monohydrate. On the basis of the analytical and spectroscopic data, the copper complex is suggested to possess an elongatedtetragonal copper (II) ions environment with d22 ground state, the complex was found to be mononuclear with respect to copper atom. The zinc complex possessed square-pyramidal geometry having coordination number 5. The complexes were found to be much more active (copper complex possessed about four times enhanced activity, zinc complex about three times higher activity) against S. aureus. Similarly copper complex possessed 14 times higher activity and zinc complex about 10 times higher activity against E. coli. This work presents a major advance to the pharmaceutical sciences. The complexes reported in this study may replace cephalexin in daily use due to their higher activities against the micro-organisms sensitive to cephalexin.
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The work presented in this thesis concerns the role of metal ions through chelation in drug design. The area received much attention since the claim that the complexes of drug substances with metal ions are more active and less toxic than the parent drug.
In this work complexes of cephalexin with copper and zinc ions were prepared and characterized by microanalysis, IR and UV-vis spectrophotometry, magnetic measurement techniques, differential scanning calorimetry, and atomic absorption spectrometry. The complexes were found to be of ML2 type where M is the metal ion and L stands for the ligand. Both the complexes were monohydrate. On the basis of the analytical and spectroscopic data, the copper complex is suggested to possess an elongatedtetragonal copper (II) ions environment with d22 ground state, the complex was found to be mononuclear with respect to copper atom. The zinc complex possessed square-pyramidal geometry having coordination number 5.

The complexes were found to be much more active (copper complex possessed about four times enhanced activity, zinc complex about three times higher activity) against S. aureus. Similarly copper complex possessed 14 times higher activity and zinc complex about 10 times higher activity against E. coli.

This work presents a major advance to the pharmaceutical sciences. The complexes reported in this study may replace cephalexin in daily use due to their higher activities against the micro-organisms sensitive to cephalexin.

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