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

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

Volume: 2 Issue: 6

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

Affiliation:

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

Abstract: 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.

Cite this article as:

Wollmann J., Molnar J. and Hilgeroth A., Physicochemical Characteristics Of Novel P-Glycoprotein Inhibitors Of The Cage Dimeric 1,4-Dihydropyridine Type, Medicinal Chemistry 2006; 2 (6) . https://dx.doi.org/10.2174/1573406410602060565