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.
Schelkun
R M
RM
Parke-Davis Pharmaceutical Research Division of Warner-Lambert Company, Ann Arbor, MI 48105, USA.
Yuen
P
P
Malone
T C
TC
Rock
D M
DM
Stoehr
S
S
Szoke
B
B
Tarczy-Hornoch
K
K
D002121:Calcium Channel Blockers / Q000138:chemical synthesis* / Q000494:pharmacology*; D002460:Cell Line; D008697:Methane / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D002121:Calcium Channel Blockers; D008697:Methane