Journal of Pharmacy and Pharmacology · 1967 · 133 citations · 7 references
PharmacyMedicinal ChemistryPharmacologyBioavailabilityMass Spectrometric AnalysisStructure-activity RelationshipsDrug DispositionDrug SolubilityIonization TechniquesIonizationLow SolubilityPh DependencePh-dependent Drug SolubilityPoorly Water-soluble DrugsSolubilitySolubility DeterminationSolubility-ph Relationships
Abstract A simple graphical method is described for deriving the ionization constants of poorly soluble organic bases from the pH dependence of the water solubility. Ionization constants and water solubilities of 13 aminoalkylphenothiazines and related drugs have been determined using this procedure. Potent tranquillizing activity in this group of compounds is shown to be associated with a low water solubility at blood pH.
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The surface activity of tranquilizers
Philip Seeman, Harvey S. Bialy · Biochemical Pharmacology · 1963 · 126 citations
Molecular Modification in Drug Design.
Alfred Burger · Journal of Medicinal Chemistry · 1965 · 59 citations