ANTIDIARRHEAL ACTIVITY OF NEW THIAZOLIDINONES RELATED TO LOPERAMIDE

A series of thiazolidinones related to loperamide was synthesized and evaluated for antidiarrhoeal activity in mice, using the castor oil te st. Of five compounds tested, antidiarrhoeal activity was found only f or 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 valu es=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 result s support the hypothesis that this compound, like loperamide, is an op iate-receptor agonist.