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ACS Med Chem Lett
; 1(9): 472-7, 2010 Dec 09.
Article
in English
| MEDLINE
| ID: mdl-24900233
ABSTRACT
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.