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J Chromatogr A. 2017 Oct 20;1520:9-22. doi: 10.1016/j.chroma.2017.09.015. Epub 2017 Sep 07.

Thin layer chromatography in drug discovery process.

Journal of chromatography. A

Krzesimir Ciura, Szymon Dziomba, Joanna Nowakowska, Michał J Markuszewski

Affiliations

  1. Department of Physical Chemistry, Faculty of Pharmacy, Medical University of Gdansk, 107 Hallera Street, 80-416 Gdansk, Poland. Electronic address: [email protected].
  2. Department of Toxicology, Faculty of Pharmacy, Medical University of Gdansk, 107 Hallera Street, 80-416 Gdansk, Poland.
  3. Department of Physical Chemistry, Faculty of Pharmacy, Medical University of Gdansk, 107 Hallera Street, 80-416 Gdansk, Poland.
  4. Department of Biopharmacy and Pharmacodynamics, Faculty of Pharmacy, Medical University of Gdansk, 107 Hallera Street, 80-416 Gdansk, Poland.

PMID: 28931459 DOI: 10.1016/j.chroma.2017.09.015

Abstract

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.

Copyright © 2017 Elsevier B.V. All rights reserved.

Keywords: Lipophilicity; Quantitative structure activity relationship; Quantitative structure retention relationship; Salting-out thin-layer chromatography; Thin layer chromatography

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