LIPOPHILICITY STUDIES ON BETA-BLOCKER BENZOXAZINONE DERIVATIVES

An investigation into the lipophilicity of a series of beta-blocker be nzoxazinone derivatives was carried out. Octanol-water partition coeff icients were determined and correlated with calculated Values accordin g to the systems of Rekker, Leo-Hansch, Ghose-Crippen and Suzuki-Kudo. Deviations are discussed. Partition coefficients were also correlated with chromatographic indices (R-Mw), obtained under different conditi ons concerning the stationary aad mobile phase. Differences in the lip ophilic behaviour observed among the systems were examined in detail. Moreover, distribution coefficients at pH 7.4 have been determined and compared to corresponding apparent R-Mw values.