Discovery ofOmecamtiv Mecarbilthe First, Selective, Small Molecule Activator of Cardiac Myosin
ACS Medicinal Chemistry Letters2010Vol. 1(9), pp. 472–477
Citations Over TimeTop 11% of 2010 papers
B. Paul Morgan, Alexander R. Muci, Pu‐Ping Lu, Xiangping Qian, Todd Tochimoto, Whitney W. Smith, Marc Garard, Erica Kraynack, Scott E. Collibee, Ion Suehiro, Adam L. Tomasi, S. Corey Valdez, Wenyue Wang, Hong Jiang, James J. Hartman, Héctor M. Rodrı́guez, Raja Kawas, Sheila Sylvester, Kathleen A. Elias, Guillermo Godinez, Kenneth Lee, Robert L. Anderson, Sandra H. Sueoka, Donghong Xu, Zhengping Wang, N. Djordjević, Fady I. Malik, David J. Morgans
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.
Related Papers
- A GEOMETRIC MEAN IN THE FURUTA INEQUALITY(2002)
- Susquehanna Chorale Spring Concert "Roots and Wings"(2017)
- Коммуникaтивно- прaгмaтический aнaлиз дипломaтических бумaг (нa основе вербaльных нот)(2018)
- → ФОРМИРОВAНИЕ ГОТОВНОСТИ БУДУЩИХ ПЕДAГОГОВ К ОРГAНИЗAЦИИ РAБОТЫ ПО РAЗВИТИЮ ВAЛЕОЛОГИЧЕСКОЙ КУЛЬТУРЫ ШКОЛЬНИКОВ(2023)