Synthesis and activity of phenyl derivatives containing 5,6-dimethylthieno[2,3-d]pyrimidin-4(1H)-one or 4H-pyrimido[5,4-b]indol-4-one heterocyclic system as potential nonsteroidal anti-inflammatory drugs.
The synthesis, the analgesic and anti-inflammatory activities of two series of phenyl derivatives containing 5,6-dimethyl-thieno[2,3-d]pyrimidin-4(1H)-one and 4H-pyrimido[5,4-b]indol-4-one system, respectively, are reported. Two of these derivatives, 6A and 9B, showed interesting activities. The results of the pharmacological assays are discussed.
Santagati
Andrea
A
Dipartimento di Scienze Farmaceutiche, Università di Catania, Catania, Italy. asantaga@mbox.unict.it
Granata
Giuseppe
G
Santagati
Maria
M
Cutuli
Vincenza
V
Mangano
Nunzio Guido
NG
Caruso
Antonina
A
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis* / Q000494:pharmacology* / Q000633:toxicity; D001522:Behavior, Animal / Q000187:drug effects; D004487:Edema / Q000139:chemically induced / Q000517:prevention & control; D006168:Guinea Pigs; D007202:Indicators and Reagents; D007211:Indoles / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D008297:Male; D010147:Pain Measurement / Q000187:drug effects; D010538:Peritonitis / Q000139:chemically induced / Q000517:prevention & control; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D011744:Pyrimidinones / Q000138:chemical synthesis* / Q000494:pharmacology* / Q000633:toxicity; D051381:Rats; D017207:Rats, Sprague-Dawley; D013055:Spectrophotometry, Infrared; D017550:Spectroscopy, Fourier Transform Infrared; D013276:Stomach Ulcer / Q000139:chemically induced
C460900:4H-pyrimido(5,4-b)indol-4-one; C460899:5,6-dimethyl-thieno(2,3-d)pyrimidin-4(1H)-one; D000894:Anti-Inflammatory Agents, Non-Steroidal; D007202:Indicators and Reagents; D007211:Indoles; D011743:Pyrimidines; D011744:Pyrimidinones