I= PREPARATION, CHARACTERIZATION AND BIOLOGICAL EVALUATION OF SCHIFF-BASE METAL COMPLEXES OF SOME DRUG SUBSTANCES
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Title of Thesis
PREPARATION, CHARACTERIZATION AND BIOLOGICAL EVALUATION OF SCHIFF-BASE METAL COMPLEXES OF SOME DRUG SUBSTANCES

Author(s)
Iftikhar Hussain Bukhari
Institute/University/Department Details
Bahauddin Zakariya University Multan/Department of Chemistry
Session
2002
Subject
Chemistry
Number of Pages
164
Keywords (Extracted from title, table of contents and abstract of thesis)
schiff bases, ligands, cu(ii), zn(ii), amoxicillin, cephalexin, sulphamethoxazole, trimethopim, salicylaldehyde, pyridoxal, amino group, salicylaldehyde, pyridoxal hydrochloride

Abstract
The work presented in this thesis concerns the preparation, characterization and biological evaluation of Cu(II) and Zn(II) complexes of Schiff bases derived from amoxicillin, cephalexin, sulphamethoxazole and trimethopim, and salicylaldehyde and pyridoxal. In these complexes an amino group available in the drug substances was allowed to react with salicylaldehyde and pyridoxal hydrochloride, separately, to obtain Schiff bases which were, subsequently, reacted with Cu(CH3CCO)2.H2O and /or Zn(CH3COO)2.2H2O to form Schiff base metal complexes. The Schiff bases prepared were: salicylideneamoxycillin, salicylidenecephalexin, salicylidenesulphamethoxazole, salicylidenetrimethoprim, pyridoxylideneamoxycillin, pyridoxylidenecephalexin, pyridoxylidene-sulphamethoxazole and pyridoxylidenetrimethoprim, and the metal complexes were: Cu(II) ā€“ and/or Zn(II) ā€“ salicylidenetrimethoprim; pyridoxylidene-amoxycillin, pyridoxylidenecephalexin, pyridoxylidensesulphamethoxazole and pyridoxylidenetrimethoprim.

The Schiff base ligands and the complexes were characterized by microanalytical, thermogravimetric, magnetic and spectroscopic data. Salicylidenesulphamethoxazole-Cu(II) monohydrate and salicylidenesulphamethoxazole-Zn(II) monohydrate were five-coordinate whereas all other complexes were found to be six-coordinate dehydrates, and ML2 type. The electron paramagnetic resonance spectral lines exhibited rhombic distortion from axial symmetry, with gā•‘ > gā”“ > ge, in the elongated-tetragonal Cu(II) complexes. The geometry of the Zn(II) complexes appears to be simple square-pyramidal or octahedral. All the compounds under investigation possess antibacterial activity. The antibacterial activity showed the following trend: Cu(II)-complexes> Zn(II)-complex>Schiff base ligands> parent drugs. The Cu(II)-Complexes with the Schiff bases derived from cephalexin showed substantially enhanced activity against P. aeruginosa as compared with the parent drug. All the copper complexes were also found to be active against Kaolin paw oedema whereas the parent drugs were inactive.

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1499.83 KB
S. No. Chapter Title of the Chapters Page Size (KB)
1 0 Contents/ Abstract
157.73 KB
2 1 Introduction 2
436.91 KB
  1.1 Schiff bases and their chemistry 2
  1.2 Biological importance of Schiff bases 3
  1.3 Schiff base transition metal complexes 4
  1.4 Chemistry and biological importance of Schiff base transition metal complexes 5
  1.5 Effect of complexation on biological activity 8
  1.6 Schiff base components under investigation 11
  1.7 Metallo -elements under investigation 24
  1.8 Schiff base transition metal complexes 29
  1.9 Aim of the work 30
  1.10 Physical techniques used for characterization 31
  1.11 Antibacterial activity 39
  1.12 Anti-inflammatory activity 43
3 2 Experimental 46
250.8 KB
  2.1 Materials 46
  2.2 Methods 48
4 3 Results and Discussion 75
736.8 KB
  3.1 Preparation of Ligands 75
  3.2 Preparation of Complexes 75
  3.3 Characterization 76
  3.4 Proposed structures 81
  3.5 Biological evaluation 134
5 4 References 151-164
126.36 KB