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New hybrid thiazolyl–pyrazoline derivatives (4a–k) were obtained through a facile and versatile synthetic procedure, and their inhibitory effects on the human carbonic anhydrase (hCA) isoforms I and II as well as on acetylcholinesterase (AChE) were determined. All new thiazolyl–pyrazolines showed activity at nanomolar levels as hCA I, hCA II, and AChE inhibitors, with K_I values in the range of 13.35–63.79, 7.01–115.80, and 17.89–48.05 nM, respectively. 1‐[4‐(4‐Cyanophenyl)thiazol‐2‐yl]‐3‐(4‐piperidinophenyl)‐5‐(4‐fluorophenyl)‐2‐pyrazoline (4f) and 1‐(4‐phenylthiazol‐2‐yl)‐3‐(4‐piperidinophenyl)‐5‐(4‐fluorophenyl)‐2‐pyrazoline (4a) against hCAs and 1‐[4‐(4‐chlorophenyl)thiazol‐2‐yl]‐3‐(4‐piperidinophenyl)‐5‐(4‐fluorophenyl)‐2‐pyrazoline (4d) and 1‐[4‐(4‐nitrophenyl)thiazol‐2‐yl]‐3‐(4‐piperidinophenyl)‐5‐(4‐fluorophenyl)‐2‐pyrazoline (4b) against AChE were identified as highly potent …