文章基本信息

标题：Synthesis, Anti-inflammatory and Antibacterial Activities of Novel Pyrazolo[4,3- g ]pteridines
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作者：Shawkat Ahmed Abdel-Mohsen ; Talaat Ibrahim El-Emary ; Hussein Salama El-Kashef 等
期刊名称：Chemical and Pharmaceutical Bulletin
印刷版ISSN：0009-2363
电子版ISSN：1347-5223
出版年度：2016
卷号：64
期号：5
页码：476-482
DOI：10.1248/cpb.c16-00044
出版社：The Pharmaceutical Society of Japan
摘要：A novel series of 6-substituted pyrazolo[3,4- g ]pteridines 2 – 9 and pyrazolo[4,3- e ][1,2,4]triazolo[1,5- c ]pteridin-2(3 H )-one (thione) 10 and 11 was synthesized using the starting compound 3,7-dimethyl-1-phenylpyrazolo[4′,3′:5,6]pyrazino[2,3- d ][1,3]oxazin-5(1 H )-one 2 . The structure of the newly synthesized compounds was elucidated by IR, ¹H-NMR, ¹³C-NMR, mass spectroscopy and elemental analyses. The anti-inflammatory activity of all the newly synthesized compounds was evaluated using the carrageenan-induced paw oedema test in rats using indomethacin as the reference drug. Compound 11 and the two derivatives 7f and 8b were the most active compounds, showing an activity comparable to indomethacin. Also, the synthesized compounds were evaluated for their antibacterial activity against Gram-positive bacteria ( Staphylococcus aureus and Bacillus cereus ) and Gram-negative bacteria ( Escherichia coli and Pseudomonas aeruginosa ) using chloramphenicol as control. The pyrazolotriazolopteridin-2-thione 11 , 6-hydroxyethyl- 6a , 6-(4-nitrophenyl)- 7g , and 6-(phenylamino) 8b derivatives were found to be the most active compounds against the Gram-positive species. None of them showed any activity against Gram-negative species.