SYNTHESIS AND LOCAL-ANESTHETIC ACTIVITY OF SOME DERIVATIVES OF LKOXYPHENYLCARBAMOYLOXY)BORNAN-3-YLMETHYL-AMMONIUM CHLORIDES

A series of 8 new esters of 2-alkoxyphenyl-carbamoic acid were synthes ized and assayed for local anesthetic activity. All compounds were iso lated as hydrochlorides and their structure was proved by H-1-NMR C-13 -NMR and IR spectroscopy. The index of anesthetic activity in infiltra tion and surface anesthesia proved that all prepared compounds are sig nificantly more active than the standard reference compounds, procaine and cocaine, respectively; it is tightly correlated with the length o f the alkoxy group. It was found that there is a parabolic relationshi p between log activity and molecular lipophilicity (as measured by R(M )). Toxicity of all compounds is within acceptable limits.