Parallel solid-Phase synthesis of zatebradine analogues as potential If channel blockers

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 μM compared to a reduction of 40% at 3 μM with zatebradine 1.