N,N-dialkyl-dipeptidylamines as novel N-type calcium channel blockers

DOI: 10.1016/S0960-894X(99)00100-6

Source and publish data:

Bioorganic and Medicinal Chemistry Letters p. 907 - 912 (1999)

Update date:2022-08-04

Topics:

Authors:

Hu, Lain-Yen

Ryder, Todd R.

Rafferty, Michael F.

Cody, Wayne L.

Lotarski, Susan M.

Miljanich, George P.

Millerman, Elizabeth

Rock, David M.

Song, Yuntao

Stoehr, Sally J.

Taylor, Charles P.

Weber, Mark L.

Szoke, Balazs G.

Vartanian, Mark G.

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Article abstract of DOI:10.1016/S0960-894X(99)00100-6

Selective N-type voltage sensitive calcium channel (VSCC) blockers have shown utility in several models of stroke and pain. We are especially interested in small molecule N-type calcium channel blockers for therapeutic use. Herein, we report a series of N,N-dialkyl-dipeptidylamines with potent functional activity at N-type VSCCs and in vivo efficacy. The synthesis, SAR, and pharmacological evaluation of this series are discussed.

Full text of DOI:10.1016/S0960-894X(99)00100-6

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