Antidiarrhoeal Activity of New Thiazolidinones Related to Loperamide

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Abstract
A series of thiazolidinones related to loperamide was synthesized and evaluated for antidiarrhoeal activity in mice, using the castor oil test. Of five compounds tested, antidiarrhoeal activity was found only for 2−(p‐nitrophenyl)−3−{3−[(4−(p‐chloro‐phenyl)‐4−hydroxy)piperidino]ethyl}‐1,3−thiazolidin−4−one. The compound was less active than loperamide (ED50 values = 48.7 (24.8−95.6) and 0.91 (0.24−3.40) mg kg−1, respectively), but was also less toxic (LD50 values = 745.9 (545.2−929.8) and 108.9 (85.5−138.7) mg kg−1, respectively). Its antidiarrhoeal activity was counteracted by naloxone. Our results support the hypothesis that this compound, like loperamide, is an opiate‐receptor agonist.