SOME UNSYMMETRICAL ALKYLARYL UREAS PREPARATION, PHYSICAL PROPERTIES AND HYPNOTIC EFFECTS

¹ From the Burroughs Wellcome and Company, U. S. A., Experimental Research Laboratories, Tuckahoe, New York

1. Twenty-nine unsymmetrical alkylaryl ureas, the majority of them new, were synthesized and their hypnotic potencies and toxicities determined by intraperitoneal injection in albino mice.

2. A series of 13 commonly used commercial hypnotics were tested in a like manner for purposes of comparison.

3. When these ureas are compared in homologous series their hypnotic potencies are seen to increase approximately two-fold for each addition of a CH₂ group in their aliphatic portion.

4. There appears to be no consistent relationship between water solubility and hypnotic potency and toxicity.

5. In general, the Heptane/Water distribution coefficients parallel hypnotic potency and toxicity.

6. The more potent unsymmetrical alkylaryl ureas are more effective in lowering surface tension.