Aminopyrazinyl derivatives: synthesis and evaluation of antiinflammatory and related activities.
Some amides, 1-substituted methylenediamines and 2-substituted thiazolidin-4-ones, all containing the aminopyrazinyl moiety, were synthesized and tested in the experimental models of acute and chronic inflammations and as potential analgesic agents. The first series of compounds are inactive, whereas the N,N'-di-(2-pyrazinyl)-methylene-diamines and the 3-(2'-pyrazinyl)-thiazolidinones 6, 7, 11, 12 and even more 16 and 17 were found to be endowed with antiinflammatory and analgesic properties and low acute toxicity, the two latter being the most interesting.
Vigorita
M G
MG
Dipartimento Farmaco-Chimico, Facoltà di Farmacia, Messina, Italy.
Grasso
S
S
Zappalà
M
M
Ottanà
R
R
Monforte
M T
MT
Barbera
R
R
Trovato
A
A
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D001169:Arthritis, Experimental / Q000188:drug therapy; D002351:Carrageenan; D004487:Edema / Q000139:chemically induced / Q000517:prevention & control; D005260:Female; D007213:Indomethacin / Q000494:pharmacology; D007928:Lethal Dose 50; D008297:Male; D051379:Mice; D010147:Pain Measurement / Q000187:drug effects; D010653:Phenylbutazone / Q000494:pharmacology; D011719:Pyrazines / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D051381:Rats; D017208:Rats, Wistar; D011930:Reaction Time / Q000187:drug effects; D013276:Stomach Ulcer / Q000139:chemically induced
D000894:Anti-Inflammatory Agents, Non-Steroidal; D011719:Pyrazines; D002351:Carrageenan; D010653:Phenylbutazone; D007213:Indomethacin