Bandarage, Upul K.; Court, John; Gao, Huai; Nanthakumar, Suganthini; Come, Jon H.; Giroux, Simon; Green, Jeremy published the artcile< ROCK inhibitors 4: Structure-activity relationship studies of 7-azaindole-based rho kinase (ROCK) inhibitors>, Electric Literature of 112-63-0, the main research area is ROCK inhibitors protein kinase A microsome hepatocyte; 7-Azaindole; Rho kinase (ROCK); Thiazole; protein kinase A (PKA).
Rho kinase (ROCK) inhibitors are of therapeutic value for the treatment of disorders such as hypertension and glaucoma, and potentially of wider use against diseases such as cancer and multiple sclerosis. We previously reported a series of potent and selective ROCK inhibitors based on a substituted 7-azaindole scaffold. Here we extend the SAR exploration of the 7-azaindole series to identify leads for further evaluation. New compounds such as 16, 17, 19, 21 and 22 showed excellent ROCK potency and protein kinase A (PKA) selectivity, combined with microsome and hepatocyte stability.
Bioorganic & Medicinal Chemistry Letters published new progress about Bioavailability. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Electric Literature of 112-63-0.
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