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  • Synthesis, analgesic, anti-inflammatory, and antimicrobial activity of some novel pyrimido[4,5-b]quinolin-4-ones.

Synthesis, analgesic, anti-inflammatory, and antimicrobial activity of some novel pyrimido[4,5-b]quinolin-4-ones.

Bioorganic & medicinal chemistry (2007-12-26)
Abdel-Rahman B A El-Gazzar, Mervat M El-Enany, Mahmoud N Mahmoud
RESUMO

Novel series of pyrimido[4,5-b]quinolines (3a-c), triazolo[4',3':1,2]pyrimido[4,5-b]-quinolines (7a-e, 9, and 14), tetrazolo[4',3':1,2]pyrimido[4,5-b]quinolin-5-one (13), [1,3]-pyrazolo[3',2':1,2]pyrimido[4,5-b]quinolines (12a and 12b), and 2-pyrazolyl-pyrimido[4,5-b]-quinolines (15, 16a, 16b, and 19) have been synthesized. Some of the new compounds were tested against various bacteria and fungi species. In addition, the analgesic and anti-inflammatory activities are reported. Compounds 8 and 9a possess high activity toward the fungi as compared with the reference drug Nystatin. The tested compounds 5 and 8 have moderate anti-inflammatory activities. Moreover compounds 5, 8, 10, and 16a, have activities higher than the reference drug in peripheral analgesic activity testing, Compounds 5, 7a, 11a, and 16a have potencies as the reference drug in central analgesic activity testing.

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Sigma-Aldrich
Ácido acetilsalicílico, ≥99.0%
Sigma-Aldrich
Indometacina, 98.0-102.0%, meets EP testing specifications
Sigma-Aldrich
Ácido acetilsalicílico, meets USP testing specifications
Sigma-Aldrich
Nalidixic acid, ≥98%
Sigma-Aldrich
Ácido acetilsalicílico, analytical standard
Sigma-Aldrich
Indometacina, meets USP testing specifications