Potent, selective and orally bioavailable dihydropyrimidine inhibitors of Rho kinase (ROCK1) as potential therapeutic agents for cardiovascular diseases

Journal of Medicinal Chemistry

Volumn 51, Issue 21, 2008, Pages 6631-6634

  Sehon, Clark A ^a   Wang, Gren Z ^a   Viet, Andrew Q ^a   Goodman, Krista B ^a   Dowdell, Sarah E ^a   Elkins, Patricia A ^b   Semus, Simon F ^b   Evans, Christopher ^a   Jolivette, Larry J ^a   Kirkpatrick, Robert B ^b   Dul, Edward ^b   Khandekar, Sanjay S ^b   Yi, Tracey ^b   Wright, Lois L ^b   Smith, Gary K ^b   Behm, David J ^a   Bentley, Ross ^a   Doe, Christopher P ^a   Hu, Erding ^a   Lee, Dennis ^a  

^a CVU CEDD ^*  (United States)

^b GLAXOSMITHKLINE   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

CYTOCHROME P450 2D6; CYTOCHROME P450 ISOENZYME; DIHYDROPYRIDONE; DIHYDROPYRIMIDINE; DIHYDROPYRIMIDINONE; INDAZOLE DERIVATIVE; RHO KINASE INHIBITOR; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; BIGINELLI REACTION; CARDIOVASCULAR DISEASE; DRUG BIOAVAILABILITY; DRUG HALF LIFE; DRUG IDENTIFICATION; DRUG POTENCY; DRUG SELECTIVITY; DRUG SYNTHESIS; HYDROGEN BOND; HYPERTENSION; IC 50; MEAN ARTERIAL PRESSURE; NONHUMAN; RAT; SINGLE DRUG DOSE; SPONTANEOUSLY HYPERTENSIVE RAT; STRUCTURE ACTIVITY RELATION;

ADENOSINE TRIPHOSPHATE; ADMINISTRATION, ORAL; ALDEHYDES; ANIMALS; CARDIOVASCULAR DISEASES; CRYSTALLOGRAPHY, X-RAY; INDAZOLES; MODELS, MOLECULAR; MOLECULAR STRUCTURE; PROTEIN KINASE INHIBITORS; PYRIMIDINES; RATS; RHO-ASSOCIATED KINASES; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 56249114886     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm8005096     Document Type: Article

References (20)

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18. Data represent the average value for two or more measurements. Standard error is typically within 2-fold of the reported mean.
19. PK data were determined from an iv/po crossover study. Pharmacokinetic parameters represent average values from three tested animals.
20. Values are reported for the iv leg of the study.