Antibiotic Bootcamp - What Makes a Good Hit - Why and How Do You Write a TPP

Dive into an in-depth exploration of antibiotic development through this comprehensive workshop from the 2017 ASM/ESCMID Conference on Drug Development to Meet the Challenge of Antimicrobial Resistance. Learn about the crucial aspects of identifying good hits and leads, and understand the importance and process of writing a Target Product Profile (TPP). Gain insights from expert discussants including Lynn Silver, Tom Dougherty, John Tomayko, and Sherman T. Waddell as they cover topics such as discovery strategies, hit generation, mechanism of action, pharmacology evaluation, screening methods, and library collections. Explore the challenges of data interpretation, false positives, and triage processes in drug development. Delve into structure-activity relationships, optimization techniques, and the importance of drug-like properties. Examine the Rule of Five, Lipinski space, and the differences between Gram-positive and Gram-negative antibacterials. Analyze real-world examples and learn about key parameters in optimization, pharmacokinetics, therapeutic index, and medicinal chemistry principles essential for successful antibiotic development.

Intro
Short Talks
Discovery Strategies
Hit Generation
Mechanism of Action
Evaluate the Pharmacology
What Did You Scream
What Was Your Screening Cell
Big Pharma Sample Collection
Libraries for Hire
Fuzzy Data
False Positives
Real Positives
The Right Way
Triage
Chemist
How much money
Common structures
Pains
Rhodamine
Computational Filters
Backlash
Structure Activity Relationship
Optimization
Increasing potency
Tractable lead
Properties
The Rule of Five
Drug Like
Lipinsky Space
Bulking Up
Natural Products
Is it good enough
Lipinski defined drug
Lipinski definition of drug
Gram positive drugs
Gram negative drugs
What is gram negative antibacterial
What is a good hit
Small molecules
Property space
Hergenrother
Lipinsky Parameters
Running through an example
Optimization parameters
Pharmacokinetics
Therapeutic Index
Chemical Design
Physical Properties
Medicinal Chemistry