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

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. 
DOI: 10.1016/j.bmcl.2010.04.020

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Cite this paper

@article{Davis2010BenzothiopheneCR, title={Benzothiophene containing Rho kinase inhibitors: Efficacy in an animal model of glaucoma.}, author={Robert Lee Davis and Mehmet Kahraman and Thomas J Prins and Yan Beaver and Travis G Cook and Jessica E Cramp and Charmagne S Cayanan and Elisabeth M M Gardiner and M. A. Mclaughlin and Abbot F. Clark and Mark R. Hellberg and Andrew K. Shiau and Stewart A Noble and Allen J Borchardt}, journal={Bioorganic & medicinal chemistry letters}, year={2010}, volume={20 11}, pages={3361-6} }