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. 1999 Jul 5;9(13):1813-8.
doi: 10.1016/s0960-894x(99)00284-x.

Multiple parallel synthesis of N,N-dialkyldipeptidylamines as N-type calcium channel blockers

T R Ryder  1 , L Y Hu, M F Rafferty, E Millerman, B G Szoke, K Tarczy-Hornoch
Affiliations

Multiple parallel synthesis of N,N-dialkyldipeptidylamines as N-type calcium channel blockers

T R Ryder et al. Bioorg Med Chem Lett. .

Abstract

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.

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