Henchoz Yveline, Guillarme Davy, Rudaz Serge, Veuthey Jean-Luc, Carrupt Pierre-Alain
Unité de Pharmacochimie, School of Pharmaceutical Sciences, University of Geneva and University of Lausanne, Quai E-Ansermet 30, Geneva, Switzerland.
J Med Chem. 2008 Feb 14;51(3):396-9. doi: 10.1021/jm7014809. Epub 2008 Jan 12.
Accurate determinations of lipophilicity indices benefit from recent advances in chromatographic sciences such as the launch of ultraperformance liquid chromatography (UPLC). The fast strategy presented here emerges as a powerful method suitable for high-throughput log P measurements of therapeutic compounds in isocratic and gradient modes. Because UPLC columns are highly stable in basic pH conditions, this approach allows a direct lipophilicity estimation of basic compounds in their neutral forms.
亲脂性指数的准确测定受益于色谱科学的最新进展,例如超高效液相色谱(UPLC)的推出。本文提出的快速策略是一种强大的方法,适用于在等度和梯度模式下对治疗性化合物进行高通量log P测量。由于UPLC柱在碱性pH条件下高度稳定,这种方法可以直接估计中性形式碱性化合物的亲脂性。