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Navigable Slide Index

1. Introduction
2. Outline
3. Introduction of resistance
4. Drug discovery process
5. Antibiotic resistance - two fundamental questions
6. Mechanisms of antibiotic action
7. Mechanisms of antibiotic resistance: efflux pumps
8. Modification of the antibiotic pharmacophore
9. Modification of the target structure
10. Targeting existing therapy and resistance
11. b-lactamase inhibition combined with antibiotic
12. Avoiding efflux pump mechanisms
13. Overcoming modification in the target structure (1)
14. Overcoming modification in the target structure (2)
15. Considerations and methods
16. Factors for consideration: target (genomic) based
17. Factors for consideration: whole cell based
18. Target (genomic) based approaches
19. "HIT" or "lead" discovery approaches
20. Fragment based drug discovery
21. HTS vs. fragment based approach
22. Modelling: ligand and structure known approach
23. The development of benzoylaminobenzolic acids
24. Modelling: structure known but ligand unknown
25. Discovery of bacterial MurD and MurE inhibitors
26. Modelling: ligand known but structure unknown
27. Virtual screening efforts
28. Target (genomic) based approaches: summary
29. Whole cell (empirical) based approaches
30. Selection of chemical starting points (1)
31. Selection of chemical starting points (2)
32. Discovery of a new class of anti-TB agent (1)
33. Discovery of a new class of anti-TB agent (2)
34. Whole cell based approaches: summary
35. 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

Series:

• Antibiotic Resistance

Categories:

• Microbiology
• Pharmaceutical Sciences

Therapeutic Areas:

• Infectious Diseases

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 April 15, 2025, from https://doi.org/10.69645/JESX5069.
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Publication History

• Published on December 31, 2009

Financial Disclosures

• Dr. Geoffrey Coxon has not informed HSTalks of any commercial/financial relationship that it is appropriate to disclose.