| 中文摘要 | 第7-12页 |
| ABSTRACT | 第12-18页 |
| Chapter 1 Recent advance in benzimidazoles as antibacterial and antifungal drugs and strategy of this thesis | 第19-55页 |
| 1.1 Introduction | 第19-20页 |
| 1.2 Recent advance in benzimidazoles as antibacterial and antifungal drugs | 第20-43页 |
| 1.2.1 Five-membered heterocycle containing benzimidazoles as antibacterial and antifungal drugs | 第21-26页 |
| 1.2.2 Six-membered heterocycle containing benzimidazoles as antibacterial and antifungal drugs | 第26-30页 |
| 1.2.3 Fused heterocycle containing benzimidazoles as antibacterial and antifungal drugs | 第30-33页 |
| 1.2.4 Benzimidazole-based metal complexes as antibacterial and antifungal drugs | 第33-35页 |
| 1.2.5 Other benzimidazoles as antibacterial and antifungal drugs | 第35-43页 |
| 1.3 Summary | 第43-44页 |
| 1.4 Strategy of this thesis | 第44-46页 |
| References | 第46-55页 |
| Chapter 2 Design and synthesis of quinolone benzimidazole hybrids and their antimicrobial study | 第55-117页 |
| 2.1 Introduction | 第55-57页 |
| 2.2 Results and discussion | 第57-77页 |
| 2.2.1 Chemistry | 第57-58页 |
| 2.2.2 Biological activity | 第58-63页 |
| 2.2.3 Bacterial resistance study | 第63-64页 |
| 2.2.4 Bactericidal kinetics study | 第64-65页 |
| 2.2.5 Cytotoxicity | 第65-66页 |
| 2.2.6 Molecular docking study | 第66-67页 |
| 2.2.7 Inhibitory activity against topoisomerase IV | 第67页 |
| 2.2.8 Quantum chemical studies | 第67-69页 |
| 2.2.9 Interactions with drug-resistant P. aeruginosa DNA | 第69-75页 |
| 2.2.10 Cleavge of drug-resistant P. aeruginosa DNA | 第75-76页 |
| 2.2.11 Bacterial membrane permeabilization | 第76-77页 |
| 2.3 Conclusions | 第77-78页 |
| 2.4 Experimental protocols | 第78-93页 |
| 2.4.1 General methods | 第78-89页 |
| 2.4.2 Antibacterial and antifungal assays | 第89-90页 |
| 2.4.3 Resistance study | 第90页 |
| 2.4.4 Bactericidal kinetic assay | 第90页 |
| 2.4.5 Cytotoxicity | 第90-91页 |
| 2.4.6 Molecular docking | 第91页 |
| 2.4.7 Quantum chemical studies | 第91页 |
| 2.4.8 The UV absorption spectra | 第91页 |
| 2.4.9 Isolating genomic DNA from P. aeruginosa bacterial strain | 第91-93页 |
| 2.4.10 P. aeruginosa DNA cleavage experiments | 第93页 |
| 2.4.11 Bacterial membrane permeabilization | 第93页 |
| References | 第93-99页 |
| APPENDIX I | 第99-117页 |
| I.1 Spectra of some representative compounds | 第99-115页 |
| I.2 This chapter was published as a cover feature in ChemMedChem | 第115-117页 |
| Chapter 3 Design and synthesis of purine benzimidazole hybrids and their antimicrobial study | 第117-185页 |
| 3.1 Introduction | 第117-119页 |
| 3.2 Results and discussion | 第119-144页 |
| 3.2.1 Chemistry | 第119-121页 |
| 3.2.2 Biological activity | 第121-126页 |
| 3.2.3 Structure?activity relationship | 第126-130页 |
| 3.2.4 Quantum chemical studies | 第130-132页 |
| 3.2.5 Cytotoxicity | 第132-133页 |
| 3.2.6 Reactive oxygen species | 第133-135页 |
| 3.2.7 Interactions with drug-resistant S. aureus DNA | 第135-139页 |
| 3.2.8 Measurement of fluorescence spectra | 第139-144页 |
| 3.3 Conclusions | 第144-145页 |
| 3.4 Experimental protocols | 第145-163页 |
| 3.4.1 General methods | 第145-158页 |
| 3.4.2 Antibacterial and antifungal assays | 第158-160页 |
| 3.4.3 Crystalline cell packing maps of purine benzimidazole containing pyrrole III–6b | 第160页 |
| 3.4.4 Cytotoxicity | 第160-161页 |
| 3.4.5 Reactive oxygen species | 第161页 |
| 3.4.6 Molecular docking | 第161页 |
| 3.4.7 Quantum chemical studies | 第161页 |
| 3.4.8 Isolating genomic DNA from S. aureus bacterial strain | 第161-162页 |
| 3.4.9 The UV absorption spectra | 第162-163页 |
| References | 第163-169页 |
| APPENDIX II | 第169-185页 |
| Spectra of some representative compounds | 第169-185页 |
| Results and prospects | 第185-189页 |
| Financial support | 第189-191页 |
| Acknowledgements | 第191-193页 |
| A brief introduction to the author | 第193-195页 |
| Achievements | 第195-196页 |
