In the search for new antiinflammatory drugs: synthesis and antiinflammatory activity of some Thiazolo(3,2-a)pyrimidine derivatives containing a thioether group.
Our strategy for the exploration of new NSAIDs starts on the synthesis of derivatives of 5-oxo-5H-Thiazolo [3,2-a] pyrimidines. The compounds were achieved by the following methods: (a) condensation of 2-amino-4-alkylthiomethilthiazole with ethyl 4-chloro-3-oxobutanoate (PPA method), (b) triphenyl phosphonium salts preparation, (c) Wittig-reaction of the salts with suitable aldehyde. Synthesized compounds were screened for antiinflammatory activity in the carrageenin rat paw oedema assay according to Winter et al. Some of the new synthesize compounds, at the dose used (50 mg/Kg) reduced meaningfully the oedema. The pharmacological effect varies according to the administration time.
Passarotti
C M
CM
Research Centre, Formenti Group, Origgio, Italy.
Valenti
M
M
Marini
M
M
D000478:Alkylation; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis* / Q000494:pharmacology; D002351:Carrageenan; D004487:Edema / Q000139:chemically induced / Q000517:prevention & control; D005260:Female; D008297:Male; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000494:pharmacology; D051381:Rats; D017208:Rats, Wistar; D013844:Thiazoles / Q000138:chemical synthesis* / Q000494:pharmacology
D000894:Anti-Inflammatory Agents, Non-Steroidal; D011743:Pyrimidines; D013844:Thiazoles; D002351:Carrageenan