Bioorganic and Medicinal Chemistry Letters p. 2351 - 2354 (2001)
Update date:2022-08-03
Topics: Solid-phase synthesis Analogues High-Throughput Screening Experimental Design Parallel Synthesis
Bom, Anton
Booth, Susan
Bruin, John
Clark, John
Miller, Susan
Wathey, Bernard
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.
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