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Estimation of phospholipophilicity of 1‐[3‐(arylpiperazin‐1‐yl)‐propyl]‐pyrrolidin‐2‐one derivatives on immobilized artificial membrane stationary phase and its correlation with biological data
Author(s) -
Kulig Katarzyna,
Malawska Barbara
Publication year - 2006
Publication title -
biomedical chromatography
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.4
H-Index - 65
eISSN - 1099-0801
pISSN - 0269-3879
DOI - 10.1002/bmc.660
Subject(s) - chemistry , chromatography , high performance liquid chromatography , membrane , synthetic membrane , biochemistry
A molecule library containing 42 1‐[3‐(arylpiperazin‐1‐yl)‐propyl]‐pyrrolidin‐2‐one derivatives has been designed and synthesized. The phospholipophilicity of the obtained compounds has been determined using immobilized artificial membrane high‐performance liquid chromatography (IAM‐HPLC). The performed analysis allowed the calculation of log k we values for each of the tested compounds. Experimental phospholipophilicity data (log k we ) has been compared with the affinity of the tested compounds to α 2 ‐adrenoceptors. Performed quantitative structure–activity relationship studies indicated that, for the tested compounds, there are dependences between affinity for α 2 ‐adrenoceptors and their log k we values. The obtained results confirmed that the applied chromatographic IAM‐HPLC method could be useful in fast characterization of the phosholipophilicity of structurally closely related compounds as well as for larger series of compounds, such as drug candidates. It could also be used as a tool for further research into this group of compounds. Copyright © 2006 John Wiley & Sons, Ltd.