✦ LIBER ✦
Substituted 2H-isoquinolin-1-ones as potent Rho-kinase inhibitors: Part 2, optimization for blood pressure reduction in spontaneously hypertensive rats
✍ Scribed by John D. Ginn; Todd Bosanac; Rhonda Chen; Charles Cywin; Eugene Hickey; Mohammed Kashem; Steven Kerr; Stanley Kugler; Xiang Li; Anthony Prokopowicz III; Sabine Schlyer; James D. Smith; Michael R. Turner; Frank Wu; Erick R.R. Young
- Book ID
- 104004630
- Publisher
- Elsevier Science
- Year
- 2010
- Tongue
- English
- Weight
- 645 KB
- Volume
- 20
- Category
- Article
- ISSN
- 0960-894X
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✦ Synopsis
Phenylglycine substituted isoquinolones 1 and 2 have previously been described as potent dual ROCK1/ROCK2 inhibitors. Here we describe the further SAR of this series to improve metabolic stability and rat oral exposure. Piperidine analog 20 which demonstrates sustained blood pressure normalization in an SHR blood pressure reduction model was identified through this effort.