J. Wollmann, J. Molnar and A. Hilgeroth Pages 565 - 568 ( 4 )
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.
P-glycoprotein, partition coefficient, cage dimer, biological activity
Institute of Pharmaceutical Chemistry, Martin-Luther-University Halle-Wittenberg, 06120 Halle, Germany.