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

…, DM Rock, S Stoehr, B Szoke, K Tarczy-Hornoch

Index: Schelkun, Robert M.; Yuen, Po-wai; Malone, Thomas C.; Rock, David M.; Stoehr, Sally; Szoke, Balazs; Tarczy-Hornoch, Katalin Bioorganic and Medicinal Chemistry Letters, 1999 , vol. 9, # 16 p. 2447 - 2452

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Citation Number: 12

Abstract

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.