2014年9月14日日曜日

Orally Bioavailable Dihydropyrimidine Inhibitors of Rho Kinase (ROCK1)

 Orally Bioavailable Dihydropyrimidine Inhibitors of Rho Kinase (ROCK1)


Abstract

Abstract Image
Recent studies using known Rho-associated kinase isoform 1 (ROCK1) inhibitors along with cellular and molecular biology data have revealed a pivotal role of this enzyme in many aspects of cardiovascular function. Here we report a series of ROCK1 inhibitors which were originally derived from a dihydropyrimidinone core 1. Our efforts focused on the optimization of dihydropyrimidine 2, which resulted in the identification of a series of dihydropyrimidines with improved pharmacokinetics and P450 properties.

Citing Articles

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This article has been cited by 8 ACS Journal articles (5 most recent appear below).
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