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Printable Handouts
Navigable Slide Index
- Introduction
- Outline
- Introduction of resistance
- Drug discovery process
- Antibiotic resistance - two fundamental questions
- Mechanisms of antibiotic action
- Mechanisms of antibiotic resistance: efflux pumps
- Modification of the antibiotic pharmacophore
- Modification of the target structure
- Targeting existing therapy and resistance
- b-lactamase inhibition combined with antibiotic
- Avoiding efflux pump mechanisms
- Overcoming modification in the target structure (1)
- Overcoming modification in the target structure (2)
- Considerations and methods
- Factors for consideration: target (genomic) based
- Factors for consideration: whole cell based
- Target (genomic) based approaches
- "HIT" or "lead" discovery approaches
- Fragment based drug discovery
- HTS vs. fragment based approach
- Modelling: ligand and structure known approach
- The development of benzoylaminobenzolic acids
- Modelling: structure known but ligand unknown
- Discovery of bacterial MurD and MurE inhibitors
- Modelling: ligand known but structure unknown
- Virtual screening efforts
- Target (genomic) based approaches: summary
- Whole cell (empirical) based approaches
- Selection of chemical starting points (1)
- Selection of chemical starting points (2)
- Discovery of a new class of anti-TB agent (1)
- Discovery of a new class of anti-TB agent (2)
- Whole cell based approaches: summary
- General summary
Topics Covered
- Overview of the drug discovery process
- Mechanisms of antibiotic action and resistance
- Modification of the antibiotic pharmacophore
- Modification of the target structure
- Targeting existing therapy and resistance mechanisms
- Overcoming modification in the target structure
- Considerations and methods in the discovery of new antibiotics
- Genomic based approaches
- Lead discovery approaches
- Fragment based drug discovery
- Modelling: ligand and structure known approach
- Modelling: structure known but ligand unknown approach
- Modelling: ligand known but structure unknown
- Whole cell (empirical) based approaches
- Selection of chemical starting points
Links
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Talk Citation
Coxon, G. (2009, December 31). Medicinal chemistry strategies in combating antibiotic resistance [Video file]. In The Biomedical & Life Sciences Collection, Henry Stewart Talks. Retrieved October 7, 2024, from https://doi.org/10.69645/JESX5069.Export Citation (RIS)
Publication History
Financial Disclosures
- Dr. Geoffrey Coxon has not informed HSTalks of any commercial/financial relationship that it is appropriate to disclose.