Biological evaluation of compounds with -NCS- group or derived from thiazole and imidazole. Activity on prostaglandin synthetase complex.
The effects of compounds with activity against thyroid peroxidase were tested on the activity of hydroperoxidase and cyclo-oxygenase of the prostaglandin synthetase complex in-vitro. Active compounds were found to inhibit the peroxidase, and the cyclo-oxygenase function. These compounds were also found to have anti-inflammatory activity as demonstrated by the reduction of carrageenan-induced oedema of the hind paw of the rat. Indomethacin and non-steroidal anti-inflammatory drugs tested under the same conditions were shown to have activity towards the cyclo-oxygenase rather than the peroxidase function of the prostaglandin synthetase complex. A common feature of the active compounds was the presence of an -NCS- linkage or free -SH group.
Moulard
T
T
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Limoges, France.
Lagorce
J F
JF
Thomas
J C
JC
Raby
C
C
D000818:Animals; D002351:Carrageenan; D016861:Cyclooxygenase Inhibitors / Q000494:pharmacology*; D004487:Edema / Q000139:chemically induced / Q000188:drug therapy; D007093:Imidazoles / Q000494:pharmacology*; D008297:Male; D010544:Peroxidases / Q000037:antagonists & inhibitors; D011451:Prostaglandin-Endoperoxide Synthases / Q000187:drug effects / Q000378:metabolism*; D051381:Rats; D017208:Rats, Wistar; D013844:Thiazoles / Q000494:pharmacology*
D016861:Cyclooxygenase Inhibitors; D007093:Imidazoles; D013844:Thiazoles; D002351:Carrageenan; D010544:Peroxidases; D011451:Prostaglandin-Endoperoxide Synthases