Po-Wai Yuen

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 VACCs over sodium and potassium channels. The methods of synthesis and preliminary pharmacology are discussed herein.

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 VACCs have been identified. Their synthesis and preliminary pharmacology are discussed herein.

N-(2-(4-hydroxyphenyl)ethyl)-4-chlorocinnamide: A novel antagonist at the 1a/2B NMDA receptor subtype

A series of N-(2-phenethyl)cinnamides was synthesized and assayed for antagonism at three N-methyl-D-asparate (NMDA) receptor subtypes (NR1A/2A-C). N-(2-(4-hydroxyphenyl)ethyl)-4-chlorocinnamide (6) was identified as a highly potent and selective antagonist of the NR1A/2B subtype.