Recently, we described the first small-molecule inhibitor,(E)-ethyl 2-cyano-3-(3, 4- dichlorophenyl) acryloylcarbamate (1), of the PDZ domain of protein interacting with Cα- kinase 1 (PICK1), a potential drug target against brain ischemia, pain and cocaine addiction. Herein, we explore structure–activity relationships of 1 by introducing subtle modifications of the acryloylcarbamate scaffold and variations of the substituents on this scaffold. The ...
