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Discovery of N-(1-adamantyl)-2-(4-alkylpiperazin-1-yl)acetamide derivatives as T-type calcium channel (Cav3.2) inhibitors |
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| Authors: | Giordanetto Fabrizio Knerr Laurent Selmi Nidhal Llinàs Antonio Lindqvist Anders Wang Qing-Dong Ståhlberg Pernilla Thorstensson Fredrik Ullah Victoria Nilsson Kristina O'Mahony Gavin Högberg Got Lindhardt Emma Strand Annika Duker Göran |
| Affiliation: | Medicinal Chemistry, AstraZeneca R&D CVGI iMed, Pepparedsleden 1, SE-431 83 M?lndal, Sweden. fabrizio.giordanetto@astrazeneca.com |
| 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. |
| Keywords: | Calcium channel inhibition Cav3.2 T-type calcium channels |
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