作者
Fedele Manna, Franco Chimenti, Adriana Bolasco, Bruna Bizzarri, Walter Filippelli, Amelia Filippelli, Luigi Gagliardi
发表日期
1999/3/1
期刊
European journal of medicinal chemistry
卷号
34
期号
3
页码范围
245-254
出版商
Elsevier Masson
简介
4,6-diaryl and 4,6-aryl-indolyl substituted 3-cyano-2-aminopyridines were synthesized and submitted to evaluation for their anti-inflammatory, analgesic and antipyretic activity. The electronegativity of the substituents and their displacement on the 4- or 6-aryl ring of the 4,6-diaryl-3-cyano-2-aminopyridine nucleus (3a–q) influenced the anti-inflammatory activity which was higher in the presence of electron-realising groups. The introduction of the indol-3-yl substituent in the 4-position of the 3-cyano-2-aminopyridine nucleus (6a–x) increased the anti-inflammatory and analgesic power, but there was no evidence of the relationship among the electronic characteristic of the substituents, their displacement on the 6-phenyl ring and the activity. Conversely, the displacement of the 2-hydroxyphenyl group in the 4-position (4a–e) and of the indol-3-yl group in the 6-position (8h–w) decreased the anti-inflammatory activity. All …
引用总数
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学术搜索中的文章
F Manna, F Chimenti, A Bolasco, B Bizzarri, W Filippelli… - European journal of medicinal chemistry, 1999