Synthesis and pharmacological evaluation of thieno[2,3-d]pyrimidin-2,4-dione and 5H-pyrimido [5,4-b]indol-2,4-dione derivatives.
Two series of novel derivatives based on the thienopyrimidine and pyrimidoindole ring systems, both N-substituted in position 3, have been synthesized. The compounds were obtained by reaction of N-amino groups of 5,6-dimethyl-thieno[2,3-d]pyrimidin-2,4-dione and of 5H-pyrimido[5,4-b]indol-2,4-dione with aromatic aldehydes. Some of these substances showed an appreciable analgesic activity, a good antiinflammatory activity, a low acute toxicity with an optimal gastric tolerance.
Santagati
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NA
Instituto di Chimica Farmaceutica e Tossicologica, Università di Catania, Italy.
Caruso
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A
Cutuli
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VM
Caccamo
F
F
D018712:Analgesics, Non-Narcotic / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis / Q000494:pharmacology; D001419:Bacteria / Q000187:drug effects; D001522:Behavior, Animal / Q000187:drug effects; D002351:Carrageenan; D003903:Deuterium; D005658:Fungi / Q000187:drug effects; D007211:Indoles / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D007249:Inflammation / Q000139:chemically induced / Q000517:prevention & control; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D051379:Mice; D008826:Microbial Sensitivity Tests; D010147:Pain Measurement / Q000187:drug effects; D010538:Peritonitis / Q000139:chemically induced / Q000517:prevention & control; D011744:Pyrimidinones / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D051381:Rats; D017207:Rats, Sprague-Dawley; D013276:Stomach Ulcer / Q000139:chemically induced / Q000473:pathology; D013876:Thiophenes / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity
D018712:Analgesics, Non-Narcotic; D000894:Anti-Inflammatory Agents, Non-Steroidal; D007211:Indoles; D011744:Pyrimidinones; D013876:Thiophenes; D002351:Carrageenan; D003903:Deuterium