Synthesis and biological evaluation of thieno[2,3-d]pyrimidine derivatives for anti-inflammatory, analgesic and ulcerogenic activity.
5-Methyl-6-phenyl-2-thioxothieno[2,3-d]pyrimidone derivative (2) reacted with hydrazonoyl chloride derivatives to afford triazolothienopyrimidones 4a-f. Also, acetone-1-(2-amino-5-isopropyl-thiophene-3-carbonitrile) (3) reacted with functional and bifunctional groups to yield the corresponding compounds 5-11. The new products showed anti-inflammatory, analgesic, and ulcerogenic activities comparable to that of indomethacin and acetylsalicylic acid, respectively.
El-Gazzar
Abdel-Rahman B A
AR
Photochemistry Department (Heterocyclic Unit), National Research Center, Dokki, Giza, Egypt.
Hussein
Hoda A R
HA
Hafez
Hend N
HN
D019342:Acetic Acid; D000700:Analgesics / Q000138:chemical synthesis / Q000494:pharmacology / Q000633:toxicity; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000138:chemical synthesis / Q000494:pharmacology / Q000633:toxicity; D001241:Aspirin / Q000494:pharmacology; D002351:Carrageenan; D004195:Disease Models, Animal; D005260:Female; D007213:Indomethacin / Q000494:pharmacology; D007249:Inflammation / Q000139:chemically induced / Q000517:prevention & control*; D008297:Male; D051379:Mice; D015394:Molecular Structure; D010146:Pain / Q000139:chemically induced / Q000503:physiopathology / Q000517:prevention & control*; D010147:Pain Measurement; D017288:Pain Threshold / Q000187:drug effects; D011725:Pyridines / Q000138:chemical synthesis / Q000494:pharmacology / Q000633:toxicity; D051381:Rats; D013276:Stomach Ulcer / Q000139:chemically induced* / Q000473:pathology; D013329:Structure-Activity Relationship
D000700:Analgesics; D000893:Anti-Inflammatory Agents; D011725:Pyridines; C446540:thienopyridine; D002351:Carrageenan; D019342:Acetic Acid; D001241:Aspirin; D007213:Indomethacin