Journal ArticleDOI
Parabolic relation between drug potency and hydrophobicity
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This article is published in Journal of Medicinal Chemistry.The article was published on 1970-11-01. It has received 148 citations till now. The article focuses on the topics: Potency.read more
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Physicochemical Profiling (Solubility, Permeability and Charge State)
TL;DR: This review will consider recent developments in physicochemical profiling used to identify candidate molecules with physical properties related to good oral absorption and focus on the emerging instrumental methods for the measurement of the physicochemical parameters Pe, S, pKa, R, log P, and log D (and their pH-profiles).
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Absorption and Drug Development: Solubility, Permeability, and Charge State
TL;DR: Partitioning Into Liposomes, Transport Model, and Some Simple Rules: A Model for Solubility and Permeability.
Journal ArticleDOI
Linear Relationships between Lipophilic Character and Biological Activity of Drugs
Corwin Hansch,William J. Dunn +1 more
TL;DR: Chloroacetaldehyde, a probable metabolite of 2-chlorc- ethanol (ethylene chlorohydrin), was studied in a number of animal systems, in in oitro hemolysis tests, and in tissue cultures to obtain a toxicity profile of the compound.
Journal ArticleDOI
Lipophilic Character and Biological Activity of Drugs II: The Parabolic Case
Corwin Hansch,John M. Clayton +1 more
TL;DR: The analyses in this review are all based on the operational definition of lipophilic character by log P from the octanol-water system, which is, of course, great advantage in using a single reference system.
Journal ArticleDOI
The History and Development of Quantitative Structure-Activity Relationships (QSARs)
TL;DR: The first investigations into the correlation of biological activities with physicochemical properties such as molecular weight and aqueous solubility began in 1841, almost 60 years before the important work of Overton and Meyer linking aquatic toxicity to lipid-water partitioning as mentioned in this paper.
Related Papers (5)
p-σ-π Analysis. A Method for the Correlation of Biological Activity and Chemical Structure
Corwin Hansch,Toshio Fujita +1 more