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Table of contents
ABSTRACT
ABSTRAK
RÉSUMÉ
ACKNOWLEDGEMENTS
APPROVAL
DECLARATION
LIST OF TABLES
LIST OF FIGURES
LIST OF SCHEMES
LIST OF APPENDICES
LIST OF ABBREVIATIONS
CHAPTER
1 INTRODUCTION
2 LITERATURE REVIEW
2.1 S-substituted dithiocarbazate
2.2 Schiff bases and metal complexes
2.3 Biological activity
2.3.1 Anticancer activity
2.3.2 Antibacterial and antifungal activity
2.3.3 Iron chelators
2.3.4 Antituberculosis activity
2.3.5 Antiamoebic activity
2.3.6 Other biological properties
2.4 Objectives
3 NON-CONJUGATED PARENTS COMPOUNDS
3.1 Introduction
3.1.1 Types of ligands systems
3.1.1.1 Tetradentate NNSS
3.1.1.2 Potentially bidentate NS or tridentate ONS ligands with an acid or ester functionality
3.1.1.3 Potentially bidentate NS or tridentate
ONS ligands with natural potent
aldehyde or ketones moieties
3.1.2 Choice of metals
3.1.2.1 Copper
3.1.2.2 Zinc
3.1.2.3 Rhenium
3.2 Methodology
3.2.1 Materials
3.2.2 Instrumentation
3.2.3 Synthesis
3.2.3.1 Macroacyclic Cu(II) system with tetradentate NNSS ligands
3.2.3.2 Open chain Cu(II) system with bidentate NS ligands with acid or ester functionality
3.2.3.3 Open chain metal system with bidentate NS ligands with natural ketone moiety
3.3 Results and Discussion
3.3.1 Synthesis
3.3.2 Characterization of metal complexes in solid state
3.3.2.1 FT-IR
3.3.2.2 Single crystal XRD description
3.3.3 Characterization of metal complexes in solution
3.3.3.1 NMR
3.3.3.2 UV-VIS
3.3.3.3 EPR
3.3.3.4 Electrochemistry
3.4 Conclusion
4 FUNCTIONALIZED COMPOUNDS
4.1 Introduction
4.1.1 Key drawbacks of metallodrugs
4.1.2 Conjugated metal complexes
4.1.2.1 Schiff base conjugates
4.1.2.2 PEGylation
4.1.2.3 Cell penetrating peptide as cell delivery vectors
4.1.2.4 Design of metal complex-conjugates
4.2 Methodology
4.2.1 Materials
4.2.2 Instrumentation
4.2.3 Synthesis
4.3 Results and Discussion
4.3.1 Synthesis
4.3.2 Characterization of ligand conjugates
4.3.2.1 NMR
4.3.2.2 MALDI-TOF-MS/ESI-MS
4.3.3 Characterization of metal-complexes conjugates
4.3.3.1 UV-VIS
4.3.3.2 LC-MS
4.3.3.3 ITC
4.3.3.4 EPR
4.3.3.5 Electrochemistry
4.4 Conclusion
5 BIOLOGICAL ACTIVITIES
5.1 Introduction
5.1.1 Mechanism of actions of antimicrobial agents and multi-drug resistance
5.1.2 Antimicrobial peptides
5.1.3 Efflux pumps and inhibitors
5.1.4 Contribution of metal complexes to the improvement of antimicrobial agents
5.2 Methodology
5.2.1 Antimicrobial testing (MIC determination)
5.2.1.1 Bacterial strains, culture media and chemicals
5.2.1.2 Determination of bacterial susceptibility
5.2.2 In vitro cytotoxicity testing
5.3 Results and Discussion
5.3.1 Antimicrobial evaluation
5.3.1.1 Macroacyclic Cu(II) system with tetradentate NNSS ligands
5.3.1.2 Open chain Cu(II) system with bidentate NS ligands with acid or ester functionality
5.3.1.3 Functionalized compounds
5.3.2 Cytotoxicity
5.4 Conclusion
6 SUMMARY AND RECOMMENDATION
REFERENCES
