| Autor: |
Sehon CA; Departments of Medicinal Chemistry, Investigative Biology, Vascular Biology, GlaxoSmithKline, 709 Swedeland Road, King of Prussia, Pennsylvania 19406, USA. clark.a.sehon@gsk.com, Wang GZ, Viet AQ, Goodman KB, Dowdell SE, Elkins PA, Semus SF, Evans C, Jolivette LJ, Kirkpatrick RB, Dul E, Khandekar SS, Yi T, Wright LL, Smith GK, Behm DJ, Bentley R, Doe CP, Hu E, Lee D |
| Jazyk: |
angličtina |
| Zdroj: |
Journal of medicinal chemistry [J Med Chem] 2008 Nov 13; Vol. 51 (21), pp. 6631-4. Date of Electronic Publication: 2008 Oct 09. |
| DOI: |
10.1021/jm8005096 |
| Abstrakt: |
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. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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