Lipophilicity of zwitterionic sulphate conjugates of tiaramide, propranolol and 4'-hydroxypropranolol.

@article{Manners1989LipophilicityOZ,
  title={Lipophilicity of zwitterionic sulphate conjugates of tiaramide, propranolol and 4'-hydroxypropranolol.},
  author={C. N. Manners and D W Payling and Dennis A. Smith},
  journal={Xenobiotica; the fate of foreign compounds in biological systems},
  year={1989},
  volume={19 12},
  pages={1387-97}
}
1. Metabolism of basic drugs may result in the formation of zwitterionic sulphate conjugates. The additional ionization introduced by the sulphate group into these compounds compared with the basic parent drug does not produce a corresponding increase in hydrophilic character. 2. Zwitterionic conjugates have constant lipophilicity between their pKa values. The opposite charges on the ionizing functional groups in this pH range appear to cancel the effect of each other on lipophilicity. 3. In… CONTINUE READING