COMPOUND 11D

COMPOUND 11D is a novel, water-soluble, semicarbazide-containing sulfonamide derivative designed as a potential anti-glaucoma drug. It functions as a highly selective inhibitor of human carbonic anhydrase II (hCA II), demonstrating an IC50 value of 14 nM for hCA II and 2086-fold selectivity over CA I. The compound exhibits favorable physicochemical properties, including very good water solubility (up to 3%) and a neutral pH in solutions, while also showing membrane permeability. Preclinical studies in a glaucomatous rabbit eye model demonstrated its ability to strongly lower intraocular pressure when applied topically. Furthermore, COMPOUND 11D has a good safety profile with low hemolysis effect, low cytotoxicity toward human corneal epithelial cells, and no significant inhibition of hERG and CYP enzymes. It also displays good liver microsomal metabolic stability and plasma stability, suggesting its potential for further development as a topical anti-glaucoma agent.