Thin layer chromatography in drug discovery process

- Traditional and unconventional TLC systems applied for lipophilicity assessment were compared.
- Application of TLC retention constants in QSAR studies for drug discovery were reviewed.
- The principles and methodology of QSRR employed for lipophilicity prediction from TLC retention data were discussed.
- Bioautography using TLC systems for drug discovery was briefly discussed.

The review is mainly focused on application of thin layer chromatography (TLC) as simple, rapid and inexpensive method for lipophilicity assessment. Among separation techniques, TLC is still one of the most popular for lipophilicity measurement. The principles and methodology of Quantitative Structure Retention Relationship (QSRR) employed to lipophilicity prediction from retention data are presented. Moreover, applications of TLC retention constants in Quantitative Structure Activity Relationship (QSAR) studies were critically overviewed. The paper concerns also bioautography as a TLC method complementary to QSAR studies. In the article, the advantages and limitations of well established and less common planar chromatography modes applied for drug discovery process were discussed.