Synthesis and structure-activity relationship of substituted 1,2,3,4-tetrahydroisoquinolines as N-type calcium channel blockers

Voltage Activated Calcium Channel (VACC) blockers have been demonstrated to have utility in the treatment of pain and stroke. A series of aminomethyl substituted isoquinolinol derivatives with potent functional activity for N-type VACCʹs have been identified. Their synthesis and preliminary pharmacology are discussed herein.