期刊
ACS MEDICINAL CHEMISTRY LETTERS
卷 1, 期 9, 页码 472-477出版社
AMER CHEMICAL SOC
DOI: 10.1021/ml100138q
关键词
Omecamtiv mecarbil; small molecule enzyme activator; cardiac myosin; systolic heart failure
We report the design, synthesis, and optimization of the first, selective activators of cardiac myosin. Starting with a poorly soluble, nitroaromatic hit compound (1), potent, selective, and soluble myosin activators were designed culminating in the discovery of omecamtiv mecarbil (24). Compound 24 is currently in clinical trials for the treatment of systolic heart failure.
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