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- Publisher
- Wiley
- Copyright
- Copyright © 1997 Wiley Subscription Services, Inc., A Wiley Company
- ISSN
- 0931-8771
- eISSN
- 1521-3838
- DOI
- 10.1002/qsar.19970160502
- Publisher site
- See Article on Publisher Site
Abstract
A series of piperazine‐ and piperidine‐analogous propafenone derivatives was synthesized and tested for their ability to modulate PGP‐mediated multidrug resistance. A good correlation between lipophilicity and activity was obtained for a set of 13 compounds. Nevertheless, 4‐hydroxy‐4‐phenylpiperidines 4a–d generally showed higher activity than predicted. A QSAR equation for the complete set of compounds was obtained when using both lipophilicity and an indicator variable for compounds 4a–d (I=1; else I = 0) or H‐bond donor strength of the 4‐hydroxy group (rcv2 = 0.90; n=17). Synthesis of aniline derivatives demonstrated that the propanolamine nitrogen interacts in protonated form. Studies on a series of diphenylalkylamines indicate, that steric factors also seem to play a role for the interaction of the nitrogen with PGP.
Journal
Quantitative Structure-Activity Relationships – Wiley
Published: Jan 1, 1997
Keywords: ; ; ;