Synthesis and pharmacological activity of 2-(substituted phenyl)-3-[2 or 3-[(4-substituted phenyl-4-hydroxy)piperidino]ethyl or propyl]-1,3-thiazolidin-4-ones.
A series of aryl-hydroxy-piperidinoalkyl-thiazolidinones was synthesized and evaluated to inhibit castor oil-induced diarrhea in mice. The dose dependent antidiarrheal activity of the most active compound 2-(p-nitrophenyl)-3-¿2-[(4-(p-chlorophenyl)-4-hydroxy)piperidino]ethyl]- 1, 3-thiazolidin-4-one (6) was counteracted by naloxone, resulting comparable with that of loperamide, a mu opiate agonist.
Diurno
M V
MV
Dipartimento di Chimica Farmaceutica e Tossicologica, Università di Napoli, Federico II, Italia.
Mazzoni
O
O
Capasso
F
F
Izzo
A A
AA
Bolognese
A
A
D000818:Animals; D000930:Antidiarrheals / Q000138:chemical synthesis / Q000494:pharmacology*; D008297:Male; D051379:Mice; D015394:Molecular Structure; D010880:Piperidines / Q000138:chemical synthesis / Q000494:pharmacology*; D013844:Thiazoles / Q000138:chemical synthesis / Q000494:pharmacology*
D000930:Antidiarrheals; D010880:Piperidines; D013844:Thiazoles