Fang, Xingang; Yin, Yan; Chen, Yen Ting; Yao, Lei; Wang, Bo; Cameron, Michael D.; Lin, Li; Khan, Susan; Ruiz, Claudia; Schroter, Thomas; Grant, Wayne; Weiser, Amiee; Pocas, Jennifer; Pachori, Alok; Schurer, Stephan; Lo Grasso, Philip; Feng, Yangbo published the artcile< Tetrahydroisoquinoline Derivatives As Highly Selective and Potent Rho Kinase Inhibitors>, Application of C10H17BN2O2, the main research area is tetrahydroisoquinoline derivative rho kinase inhibitor antiglaucoma.
Rho kinase (ROCK) is a promising drug target for the treatment of many diseases including hypertension, multiple sclerosis, cancer, and glaucoma. The structure-activity relationships (SAR) around a series of tetrahydroisoquinolines were evaluated utilizing biochem. and cell-based assays to measure ROCK inhibition. These novel ROCK inhibitors possess high potency, high selectivity, and appropriate pharmacokinetic properties for glaucoma applications. The lead compound, 35, had subnanomolar potency in enzyme ROCK-II assays as well as excellent cell-based potency (IC50 = 51 nM). In a kinase panel profiling, 35 had an off-target hit rate of only 1.6% against 442 kinases. Pharmacol. studies showed that compound 35 was efficacious in reducing intraocular pressure (IOP) in rats with reasonably long duration of action. These results suggest that compound 35 may serve as a promising agent for further development in the treatment of glaucoma.
Journal of Medicinal Chemistry published new progress about Antiglaucoma agents. 936250-20-3 belongs to class pyrazoles-derivatives, and the molecular formula is C10H17BN2O2, Application of C10H17BN2O2.
Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics