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Medicinal Chemistry


ISSN (Print): 1573-4064
ISSN (Online): 1875-6638

Physicochemical Characteristics Of Novel P-Glycoprotein Inhibitors Of The Cage Dimeric 1,4-Dihydropyridine Type

Author(s): J. Wollmann, J. Molnar and A. Hilgeroth

Volume 2 , Issue 6 , 2006

Page: [565 - 568] Pages: 4

DOI: 10.2174/1573406410602060565

Price: $65


Physicochemical characteristics of two structurally different cage dimeric 1,4-dihydropyridines HX (1) and CC (2) have been determined and compared to their P-glycoprotein inhibiting properties. While the weakly basic compound (1) showed pH-dependent apparent partition coefficients (log D), the neutral compound (2) proved to have almost identical log D values at varying pH-values. The subsequent determination of partition coefficients (log P) resulted in comparably low log P values revealing a less lipophilic compound character. Determined significantly differing P-glycoprotein (P-gp) inhibitory properties indicated that the lipophilicity of the compounds does not play a decisive role for the P-gp activity.

Keywords: P-glycoprotein, partition coefficient, cage dimer, biological activity

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