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Synthesis And Evaluation Of Biological Properties Of Derivatives Of Cephalosporins

By: Rehmat Ullah, Major | Dr.Muhammad Sabir.
Contributor(s): Dr.Haji Ahmad | Dr.Muhammad Raziq Ali.
Material type: materialTypeLabelBookPublisher: 1999Subject(s): Department of Pharmaoclogy & ToxicologyDDC classification: 0602,T Dissertation note: This study was aimed at preparation and evaluation of the biological properties of cephradine. Schiff base transition metal complexes of cephradine were prepared. In the first step Schiff bases were prepared by condensation of the primary amine with a carbonyl compound. For this purpose pyridoxal HCI and salicylaldehyde were used. In the next step the prepared Schiff bases were chelated with metal salts using copper acetate and zinc acetate, here metal binds to polydenate ligands to form the ring structure, where metal is the part of the ring. In this way a three dimensional molecule was obtained which exhibited enhanced antibacterial activity in some cases and depressed activity in the others. The complexes were subjected to biological evaluation to find out the minimum lethal concentration of the new complexes and then it was compared with the parent drug. The standard organisms of S. aureus, .E.coli Pseudomonas aeruginosa and . pneumoniae were used to study the antimicrobial activity. Cephradine complexes showed a depressed activity against S. aureus, . E.coli and P . aemginosa. But the activity of CPC and CSC derivatives was found ten times enhanced against K. pneumoniae, when compared with the present drug. The haematological study revealed that the parent drug and the new derivatives did not have any deleterious effect upon the total erythrocyte count, haemoglobin concentration, leukocytic count, differential leukocytic count i.e., lymphocytes and polyrnorphs (neutrophils). Thus the new compounds were found to be as safe as the parent drug itself.
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Veterinary Science 0602,T (Browse shelf) Available 0602,T
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This study was aimed at preparation and evaluation of the biological properties of cephradine. Schiff base transition metal complexes of cephradine were prepared. In the first step Schiff bases were prepared by condensation of the primary amine with a carbonyl compound. For this purpose pyridoxal HCI and salicylaldehyde were used. In the next step the prepared Schiff bases were chelated with metal salts using copper acetate and zinc acetate, here metal binds to polydenate ligands to form the ring structure, where metal is the part of the ring. In this way a three dimensional molecule was obtained which exhibited enhanced antibacterial activity in some cases and depressed activity in the others. The complexes were subjected to biological evaluation to find out the minimum lethal concentration of the new complexes and then it was compared with the parent drug. The standard organisms of S. aureus, .E.coli Pseudomonas aeruginosa and . pneumoniae were used to study the antimicrobial activity. Cephradine complexes showed a depressed activity against S. aureus, . E.coli and P . aemginosa. But the activity of CPC and CSC derivatives was found ten times enhanced against
K. pneumoniae, when compared with the present drug. The haematological study revealed that the parent drug and the new derivatives did not have any deleterious effect upon the total erythrocyte count, haemoglobin concentration, leukocytic count, differential leukocytic count i.e., lymphocytes and polyrnorphs (neutrophils). Thus the new compounds were found to be as safe as the parent drug itself.

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