hBChE-IN-4 (compound 40) is a potent hCA activator and BChE inhibitor with K A values of 266, 76.9, 918, 893, 98.0 nM for hCA I, hCA II, hCA IV, hCA VB, hCA VII, IC 50 values of 72.1, 4.2 nM for eeAChE, eqBChE, respectively. hBChE-IN-4 shows no cytotoxicity. hBChE-IN-4 shows potent procognitive effects. hBChE-IN-4 has the potential for the research of neurodegenerative diseases and other neuropsychiatric disorders.