Structure-activity relationship of N-methyl-N-aralkyl-peptidylamines as novel N-type calcium channel blockers
| Autor: | David J. Dooley, Charles Taylor, David M. Rock, Sally J. Stoehr, Lain-Yen Hu, George P. Miljanich, Elizabeth Millerman, Joann J. Geer, Susan M. Lotarski, Mark G. Vartanian, Balazs G. Szoke, Michael Francis Rafferty, R. Todd Ryder |
|---|---|
| Rok vydání: | 1999 |
| Předmět: |
Stereochemistry
medicine.drug_class Clinical Biochemistry Pharmaceutical Science Carboxamide N-type calcium channel Biochemistry Chemical synthesis Mice Structure-Activity Relationship In vivo Seizures Drug Discovery medicine Tumor Cells Cultured Structure–activity relationship Animals Humans Molecular Biology Voltage-dependent calcium channel Chemistry Calcium channel Organic Chemistry Dipeptides Calcium Channel Blockers Small molecule Disease Models Animal Molecular Medicine Calcium Channels |
| Zdroj: | Bioorganicmedicinal chemistry letters. 9(15) |
| ISSN: | 0960-894X |
| Popis: | Selective N-type voltage sensitive calcium channel (VSCC) blockers have shown efficacy in several animal models of stroke and pain. In the process of searching for small molecule N-type calcium channel blockers, we have identified a series of N-methyl-N-aralkyl-peptidylamines with potent functional activity at N-type VSCCs. The most active compound discovered in this series is PD 173212 (11, IC50 = 36 nM in the IMR-32 assays). SAR and pharmacological evaluation of this series are described. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|
Full Text from ScienceDirect