Chroman-3-amides as potent Rho kinase inhibitors.
Inhibition of Rho kinase (ROCK) is an attractive strategy for the treatment of diseases such as hypertension, glaucoma, and cancer. Here we report chroman-3-amides as highly potent ROCK inhibitors with sufficient kinase selectivity, excellent cell activity, good microsomal stability, and desirable pharmacokinetic properties for study as potential therapeutic agents.
Chen
Yen Ting
YT
Department of Molecular Therapeutics, The Scripps Research Institute, Florida, 130 Scripps Way, #2A1, Jupiter, FL 33458, USA.
Bannister
Thomas D
TD
Weiser
Amiee
A
Griffin
Evelyn
E
Lin
Li
L
Ruiz
Claudia
C
Cameron
Michael D
MD
Schürer
Stephan
S
Duckett
Derek
D
Schröter
Thomas
T
LoGrasso
Philip
P
Feng
Yangbo
Y
D000577:Amides / Q000138:chemical synthesis* / Q000493:pharmacokinetics*; D000818:Animals; D002626:Chemistry, Pharmaceutical / Q000379:methods; D002839:Chromans / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D015195:Drug Design; D005901:Glaucoma / Q000188:drug therapy*; D006801:Humans; D020128:Inhibitory Concentration 50; D008956:Models, Chemical; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D051381:Rats; D013997:Time Factors; D054460:rho-Associated Kinases / Q000037:antagonists & inhibitors*
D000577:Amides; D002839:Chromans; D047428:Protein Kinase Inhibitors; D054460:rho-Associated Kinases