Correlation of biological activity and high-pressure liquid chromatographic retention index for a series of propranolol, barbiturate, and anthranilic acid analogues.
The antiarrhythmic activity of propranolol analogues, the inotropic activity of propranolol analogues, the anti-inflammatory activity of anthranilic acids, the hypnotic activity of barbiturates, and the inhibition of cell division by barbiturates were correlated with either octanol--water partition coefficients or with high-pressure liquid chromatographic retention indices. The retention index, which was a scale based on the relative retention of the drug and a series of C3--C23 2-ketoalkanes, was found to give higher correlations with biological activity than was found between octanol--water partition coefficients and biological activity. Only in the case of the anthranilic acids was the retention index found to give the lower correlation.
D000818:Animals; D000889:Anti-Arrhythmia Agents; D000893:Anti-Inflammatory Agents; D001463:Barbiturates / Q000032:analysis / Q000494:pharmacology*; D002455:Cell Division / Q000187:drug effects; D002851:Chromatography, High Pressure Liquid; D066298:In Vitro Techniques; D009200:Myocardial Contraction / Q000187:drug effects; D011433:Propranolol / Q000031:analogs & derivatives* / Q000032:analysis / Q000494:pharmacology; D011817:Rabbits; D051381:Rats; D012890:Sleep / Q000187:drug effects; D012995:Solubility; D062367:ortho-Aminobenzoates / Q000032:analysis / Q000494:pharmacology*
D000889:Anti-Arrhythmia Agents; D000893:Anti-Inflammatory Agents; D001463:Barbiturates; D062367:ortho-Aminobenzoates; D011433:Propranolol