Author/Authors :
E. Hampton Sessions، نويسنده , , Wen-Yan Yin، نويسنده , , Thomas D. Bannister، نويسنده , , Amiee Weiser، نويسنده , , Evelyn Griffin، نويسنده , , Jennifer Pocas، نويسنده , , Michael D. Cameron، نويسنده , , Claudia Ruiz، نويسنده , , Li Lin، نويسنده , , Stephan C. Schürer، نويسنده , , Thomas Schroter، نويسنده , , Philip LoGrasso، نويسنده , , Yangbo Feng، نويسنده ,
Abstract :
Inhibitors of Rho kinase have been developed based on two distinct scaffolds, benzimidazoles, and benzoxazoles. SAR studies and efforts to optimize the initial lead compounds are described. Novel selective inhibitors of ROCK-II with excellent potency in both enzyme and cell-based assays were obtained. These inhibitors possess good microsomal stability, low cytochrome P-450 inhibitions and good oral bioavailability.
Keywords :
Chroman , Pyrazole , Aminopyrimidine , Rock-II , Rho kinase , Glaucoma , hypertension , Benzimidazole , Benzoxazole
