Multiple parallel synthesis of N,N-dialkyldipeptidylamines as N-type calcium channel blockers.
Selective N-type Voltage Sensitive Calcium Channel (VSCC) blockers have shown utility in several models of stroke and pain. A series of N,N-dialkyldipeptidylamines with potent functional activity at N-type VSCC's has been identified. Multiple parallel synthesis of a focused array of thirty compounds using polymer-supported quenching reagents and preliminary pharmacology are presented. Eighteen compounds were identified with an IC50 below 1 microM in an in vitro functional assay.
Ryder
T R
TR
Department of Chemistry, Parke-Davis Pharmaceutical Research, Division of Warner-Lambert Company, Ann Arbor, MI 48105, USA.
Hu
L Y
LY
Rafferty
M F
MF
Millerman
E
E
Szoke
B G
BG
Tarczy-Hornoch
K
K
D000588:Amines / Q000138:chemical synthesis*; D002121:Calcium Channel Blockers / Q000138:chemical synthesis*; D004151:Dipeptides / Q000138:chemical synthesis*; D020128:Inhibitory Concentration 50
D000588:Amines; D002121:Calcium Channel Blockers; D004151:Dipeptides; C121649:PD 151307; C121650:PD 173212