CORRELATION OF BIOLOGICAL-ACTIVITY AND HIGH-PRESSURE LIQUID-CHROMATOGRAPHIC RETENTION INDEX FOR A SERIES OF PROPRANOLOL, BARBITURATE, AND ANTHRANILIC ACID ANALOGS

The antiarrhythmic activity of propranolol analogs [in rabbit atrium], the inotropic activity of propranolol analogs, the antiinflammatory activity of anthranilic acids [in rat paw edema], 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, gave 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.