3-Arylsulphonyl-5-arylamino-1,3,4-thiadiazol-2(3H)ones as anti-inflammatory and analgesic agents.
Two series of 3-arylsulphonyl-5-arylamino-1,3,4-thiadiazol-2(3H)ones 2 with potential anti-inflammatory and analgesic activity were prepared and tested. Pharmacological results revealed that all the title compounds, endowed with an arylsulphonyl side chain, possess good antalgic activity and fair anti-inflammatory properties. The analgesic profile of the two series, evaluated by the acetic acid writhing test, showed that compounds 2c, 2f and 2h, in particular, were the most active. Structure-activity relationships are briefly discussed.
Schenone
S
S
Dipartimento di Scienze Farmaceutiche, Facoltà di Farmacia dell'Università degli Studi di Genova, Genoa, Italy. schensil@unige.it
Bruno
O
O
Ranise
A
A
Bondavalli
F
F
Filippelli
W
W
Falcone
G
G
Giordano
L
L
Vitelli
M R
MR
D000700:Analgesics / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use; D004195:Disease Models, Animal; D004487:Edema / Q000188:drug therapy; D005260:Female; D008297:Male; D051379:Mice; D010146:Pain / Q000188:drug therapy; D051381:Rats; D013457:Sulfur Compounds / Q000138:chemical synthesis* / Q000737:chemistry; D013844:Thiazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
D000700:Analgesics; D000893:Anti-Inflammatory Agents; D013457:Sulfur Compounds; D013844:Thiazoles