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- Title
Structure-Lipophilicity Relationships of Neutral and Protonated β-Blockers, Part I, Intra- and Intermolecular Effects in Isotropic Solvent Systems.
- Authors
Caron, Giulia; Steyaert, Guillaume; Pagliara, Alessandra; Reymond, Frédéric; Crivori, Patrizia; Gaillard, Patrick; Carrupt, Pierre-Alain; Avdeef, Alex; Comer, John; Box, Karl J.; Girault, Hubert H.; Testa, Bernard
- Abstract
The objectives of this study were to validate new experimental techniques used to measure the log P of protonated drugs, and to investigate the inter- and intramolecular forces influencing the partitioning behavior of β-blockers in isotropic biphasic solvent systems. The lipophilicity parameters of a number of β-blockers were measured by two-phase titration, centrifugal partition chromatography (CPC), and cyclic voltammetry (CV) in one or more of the following solvent systems: octanol/water, 1,2-dichloroethane/water, and dibutyl ether/water. CV proved to be a promising technique for measuring the lipophilicity of protonated β-blockers. Derived parameters such as Δlog P (difference between log P in two different solvent systems, a parameter valid for a given solute in a given electrical form) and diff (difference between log P of two different electrical forms of a given solute, in the same system) yielded insights into inter- and intramolecular interactions characteristic of β-blockers. The relevance of these parameters in structure-permeation relationships is explored.
- Publication
Helvetica Chimica Acta, 1999, Vol 82, Issue 8, p1211
- ISSN
0018-019X
- Publication type
Article
- DOI
10.1002/(SICI)1522-2675(19990804)82:8<1211::AID-HLCA1211>3.0.CO;2-K