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09:32
A New Straightforward Method for Lipophilicity (logP) Measurement using 19F NMR Spectroscopy
Published on: January 30, 2019
Lipophilicity in drug discovery.
1AstraZeneca, CVGI Medicinal Chemsitry, Mereside, Alderley Park, Macclesfield, Cheshire, SK10 4TG, UK +44 1625 230942 ; +44 1625 516667 ; mike.j.waring@astrazeneca.com.
Expert Opinion on Drug Discovery
|July 25, 2012
Summary
Optimal lipophilicity (logD between 1 and 3) is crucial for drug development success. Maintaining this balance enhances drug properties and increases the likelihood of successful candidate progression.
Area of Science:
- Medicinal Chemistry
- Drug Discovery
- Computational Chemistry
Background:
- Lipophilicity is a critical determinant of drug candidate quality.
- Optimal lipophilicity influences pre-clinical ADMET properties and overall development success.
- Recent advancements highlight the importance of lipophilicity in drug development.
Purpose of the Study:
- To review methods for predicting lipophilicity.
- To analyze the relationship between lipophilicity and ADMET parameters.
- To define the optimal lipophilicity range for drug development.
Main Methods:
- Literature review of lipophilicity prediction methods.
- Analysis of studies linking lipophilicity to ADMET properties.
- Synthesis of data on compound quality and lipophilicity.
Main Results:
- The optimal lipophilicity range (logD) is narrow, approximately 1 to 3.
- Operating outside this optimal range presents specific risks and challenges.
- Medicinal chemistry optimization strategies are influenced by lipophilicity.
Conclusions:
- A logD range of 1-3 represents the optimal lipophilicity space for drug candidates.
- Understanding and controlling lipophilicity is key for successful drug optimization.
- Deviations from the optimal lipophilicity range can negatively impact drug development.
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