Synthesis and SAR studies of a novel series of T-type calcium channel blockers
| Autor: | Yoonjee Kim, Min Joo Lee, Seong Jun Park, Bong Young Chung, Jae Yeol Lee, Hyewhon Rhim, Jung-Ha Lee, Sung Jun Park |
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| Rok vydání: | 2006 |
| Předmět: |
Stereochemistry
Clinical Biochemistry Quantitative Structure-Activity Relationship Pharmaceutical Science Biochemistry Chemical synthesis Cell Line Lethal Dose 50 Calcium Channels T-Type Calcium Channels N-Type Drug Discovery medicine Humans Channel blocker Molecular Biology Cells Cultured Sulfonamides Quinazoline derivatives Mibefradil Molecular Structure Chemistry Organic Chemistry T-type calcium channel Calcium Channel Blockers Electrophysiology Quinazolines Molecular Medicine Selectivity medicine.drug |
| Zdroj: | Bioorganic & Medicinal Chemistry. 14:3502-3511 |
| ISSN: | 0968-0896 |
| DOI: | 10.1016/j.bmc.2006.01.005 |
| Popis: | For the novel, potent, and selective T-type Ca 2+ channel blockers, a series of sulfonamido-containing 3,4-dihydroquinazoline derivatives were prepared and evaluated for their blocking actions on T- and N-type Ca 2+ channels. Among them, 9c ( KYS05064 , IC 50 = 0.96 ± 0.22 μM) was found to be as potent as Mibefradil and also showed the highest selectivity for T-type Ca 2+ channel with no effect on N-type Ca 2+ channel. |
| Databáze: | OpenAIRE |
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