Discovery of Omecamtiv Mecarbil the First, Selective, Small Molecule Activator of Cardiac Myosin
BP Morgan, A Muci, PP Lu, X Qian… - ACS medicinal …, 2010 - ACS Publications
ACS medicinal chemistry letters, 2010•ACS Publications
We report the design, synthesis, and optimization of the first, selective activators of cardiac
myosin. Starting with a poorly soluble, nitro-aromatic 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.
myosin. Starting with a poorly soluble, nitro-aromatic 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.
We report the design, synthesis, and optimization of the first, selective activators of cardiac myosin. Starting with a poorly soluble, nitro-aromatic 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.
ACS Publications