Antiinflammatory pyrazolones and pyrazolidones: a study of their inhibition of 5 beta-dihydrocortisone reduction in rat liver cytosol.
Seven pyrazolone and pyrazolidone derivates, some of them widely used as analgesic and anti-inflammatory drugs, were tested for the inhibitory property of the 3 alpha-hydroxysteroid dehydrogenase of rat liver cytosol. The data obtained clearly show that, among pyrazolone and pyrazolidone derivates, the correlation between IC50 and therapeutic potency is not always verified.
Schillaci
D
D
Dipartimento di Chimica e Tecnologie Farmaceutiche, Universita di Palermo, Italy.
Maggio
B
B
Raffa
D
D
Daidone
G
G
D015096:3-Hydroxysteroid Dehydrogenases / Q000037:antagonists & inhibitors; D045002:3-alpha-Hydroxysteroid Dehydrogenase (B-Specific); D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000494:pharmacology*; D003600:Cytosol / Q000187:drug effects / Q000201:enzymology / Q000378:metabolism*; D006854:Hydrocortisone / Q000031:analogs & derivatives* / Q000378:metabolism; D066298:In Vitro Techniques; D008099:Liver / Q000187:drug effects / Q000201:enzymology / Q000378:metabolism*; D011720:Pyrazoles / Q000494:pharmacology*; D051381:Rats
D000894:Anti-Inflammatory Agents, Non-Steroidal; D011720:Pyrazoles; C018921:5-dihydrocortisol; D015096:3-Hydroxysteroid Dehydrogenases; D045002:3-alpha-Hydroxysteroid Dehydrogenase (B-Specific); D006854:Hydrocortisone