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Discovery of N-(1-adamantyl)-2-(4-alkylpiperazin-1-yl)acetamide derivatives as T-type calcium channel (Cav3.2) inhibitors.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2011 Sep 15; Vol. 21 (18), pp. 5557-61. Date of Electronic Publication: 2011 Jun 30. - Publication Year :
- 2011
-
Abstract
- Chemical evolution of a HTS-based fragment hit resulted in the identification of N-(1-adamantyl)-2-[4-(2-tetrahydropyran-4-ylethyl)piperazin-1-yl]acetamide, a novel, selective T-type calcium channel (Ca(v)3.2) inhibitor with in vivo antihypertensive effect in rats.<br /> (Copyright © 2011 Elsevier Ltd. All rights reserved.)
- Subjects :
- Acetamides chemical synthesis
Acetamides chemistry
Animals
Antihypertensive Agents chemical synthesis
Antihypertensive Agents chemistry
Dose-Response Relationship, Drug
Ether-A-Go-Go Potassium Channels antagonists & inhibitors
Ether-A-Go-Go Potassium Channels metabolism
High-Throughput Screening Assays
Humans
Molecular Structure
Rats
Stereoisomerism
Structure-Activity Relationship
Acetamides pharmacology
Antihypertensive Agents pharmacology
Calcium Channels, T-Type metabolism
Drug Discovery
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 21
- Issue :
- 18
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 21782423
- Full Text :
- https://doi.org/10.1016/j.bmcl.2011.06.092