Title of article :
Thioether benzenesulfonamide inhibitors of carbonic anhydrases II and IV: Structure-based drug design, synthesis, and biological evaluation Original Research Article
Author/Authors :
William Vernier، نويسنده , , Wesley Chong، نويسنده , , David Rewolinski، نويسنده , , Samantha Greasley، نويسنده , , Thomas Pauly، نويسنده , , Morena Shaw، نويسنده , , Dac Dinh، نويسنده , , Rose Ann Ferre، نويسنده , , Seiji Nukui، نويسنده , , Martha Ornelas، نويسنده , , Eric Reyner، نويسنده ,
Abstract :
A novel series of potent thioether benzenesulfonamide inhibitors of carbonic anhydrases II and IV was discovered using structure-based drug design. Synthesis, structure–activity relationship, and optimization of physicochemical properties are described. Low nanomolar potency was achieved, and selected compounds with improved thermodynamic solubility showed promising in vitro inhibition of carbonic anhydrase activity in rabbit iris ciliary body homogenate.
