Benzothiophene containing Rho kinase inhibitors: Efficacy in an animal model of glaucoma.

ID: ALA1155477

Journal: Bioorg Med Chem Lett

Title: Benzothiophene containing Rho kinase inhibitors: Efficacy in an animal model of glaucoma.

Authors: Davis RL, Kahraman M, Prins TJ, Beaver Y, Cook TG, Cramp J, Cayanan CS, Gardiner EM, McLaughlin MA, Clark AF, Hellberg MR, Shiau AK, Noble SA, Borchardt AJ.

Abstract: We identified a new benzothiophene containing Rho kinase inhibitor scaffold in an ultra high-throughput enzymatic activity screen. SAR studies, driven by a novel label-free cellular impedance assay, were used to derive 39, which substantially reduced intraocular pressure in a monkey model of glaucoma-associated ocular hypertension.

CiteXplore: 20434334

DOI: 10.1016/j.bmcl.2010.04.020

Patent ID: ┄