Discovery of Substituted 4-(Pyrazol-4-yl)-phenylbenzodioxane-2-carboxamides as Potent and Highly Selective Rho Kinase (ROCK-II) Inhibitors.

[摘要]：The identification of a new class of potent and selective ROCK-II inhibitors is presented. Compd. SR-3677 (I) had an IC50 of ~3 nM in enzyme and cell based assays and had an off-target hit rate of 1.4% against 353 kinases, and inhibited only 3 out of 70 nonkinase enzymes and receptors. Pharmacol. studies showed that I was efficacious in both, increasing ex vivo aq. humor outflow in porcine eyes and inhibiting myosin light chain phosphorylation.

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