Thin layer chromatography in drug discovery process

被引:66
|
作者
Ciura, Krzesimir [1 ]
Dziomba, Szymon [2 ]
Nowakowska, Joanna [1 ]
Markuszewski, Michal J. [3 ]
机构
[1] Med Univ Gdansk, Dept Phys Chem, Fac Pharm, 107 Hallera St, PL-80416 Gdansk, Poland
[2] Med Univ Gdansk, Dept Toxicol, Fac Pharm, 107 Hallera St, PL-80416 Gdansk, Poland
[3] Med Univ Gdansk, Dept Biopharm & Pharmacodynam, Fac Pharm, 107 Hallera St, PL-80416 Gdansk, Poland
关键词
Lipophilicity; Quantitative structure activity relationship; Quantitative structure retention relationship; Salting-out thin-layer chromatography; Thin layer chromatography; STRUCTURE-RETENTION RELATIONSHIPS; MICELLAR LIQUID-CHROMATOGRAPHY; ACTIVITY-RELATIONSHIP ASSAY; REVERSED-PHASE; IN-SILICO; LIPOPHILICITY DETERMINATION; H-1-ANTIHISTAMINE ACTIVITY; BENZOTHIAZOLE DERIVATIVES; CONNECTIVITY INDEXES; CHEMOMETRIC ANALYSIS;
D O I
10.1016/j.chroma.2017.09.015
中图分类号
Q5 [生物化学];
学科分类号
071010 ; 081704 ;
摘要
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. (C) 2017 Elsevier B.V. All rights reserved.
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页码:9 / 22
页数:14
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