Synthesis and biological activity of substituted bis-(4-hydroxyphenyl)methanes as N-type calcium channel blockers

Voltage activated calcium channel (VACC) blockers have been demonstrated to have utility in the treatment of stroke and pain. A series of aminomethyl substituted phenol derivatives has been identified with good functional activity and selectivity for N-type VACC's over sodium and potassium channels. The methods of synthesis and preliminary pharmacology are discussed herein. A series of aminomethyl substituted phenol derivatives has been identified with good functional activity and selectivity for N-type Voltage Activated Calcium Channel over sodium and potassium channels. The methods of synthesis and preliminary pharmacology are discussed herein.