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The History of Drug Research: From Overton to Hansch

1992; Wiley; Volume: 11; Issue: 2 Linguagem: Inglês

10.1002/qsar.19920110214

1521-3838

R. F. Rekker,

Pharmaceutical Economics and Policy

Abstract The paper overviews part of the history of Drug Research, the period from Overton to and including Hansch, and pays special attention to the development of parameter sets describing electronic, lipophilic and steric substituent effects. Extra emphasis is given to the evolution in the methodology of log P calculation. The sequence of π, f (Rekker – original), f (Hansch), f (Rekker – revised) is not yet closed but open for further developments, such as development of hydrophobic fragmental sets especially designed for the study of blood‐brain barrier transfer.