Open AccessAntidiarrhoeal Activity of New Thiazolidinones Related to Loperamide
Author(s) -
Diurno M. V.,
Izzo A. A.,
Mazzoni O.,
Bolognese A.,
Capasso F.
Publication year - 1996
Publication title -
journal of pharmacy and pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.745
H-Index - 118
eISSN - 2042-7158
pISSN - 0022-3573
DOI - 10.1111/j.2042-7158.1996.tb03966.x
Subject(s) - antidiarrhoeal , loperamide , (+) naloxone , opiate , pharmacology , agonist , medicine , chemistry , traditional medicine , castor oil , opioid , receptor , biochemistry , diarrhea
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.