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Parallel solid-phase synthesis of zatebradine analogues as potential I(f) channel blockers
1Pharmacology Department, Organon Laboratories Ltd, Newhouse, Lanarkshire, ML1 5SH, Scotland, UK.
Bioorganic & Medicinal Chemistry Letters
|August 31, 2001
Abstract:
The first solid-phase synthesis of zatebradine 1 and its analogues is reported. This has resulted in the preparation of compounds with increased ability to reduce the spontaneous beating of isolated guinea-pig atria in a concentration-dependent manner. One example, 8g, showed a maximum reduction of beating of 80% at 3 microM compared to a reduction of 40% at 3 microM with zatebradine 1.