Anti-inflammatory, analgesic and antipyretic 4,6-disubstituted 3-cyano-2-aminopyridines

Citation
F. Manna et al., Anti-inflammatory, analgesic and antipyretic 4,6-disubstituted 3-cyano-2-aminopyridines, EUR J MED C, 34(3), 1999, pp. 245-254
Citations number
12
Categorie Soggetti
Chemistry & Analysis
Journal title
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
ISSN journal
02235234 → ACNP
Volume
34
Issue
3
Year of publication
1999
Pages
245 - 254
Database
ISI
SICI code
0223-5234(199903)34:3<245:AAAA43>2.0.ZU;2-2
Abstract
4,6-diaryl and 4,6-aryl-indolyl substituted 3-cyano-2-aminopyridines were s ynthesized and submitted to evaluation for their anti-inflammatory, analges ic 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-ami nopyridine nucleus (3a-q) influenced the anti-inflammatory activity which w as 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-aminopyridin e nucleus (6a-x) increased the anti-inflammatory and analgesic power, but t here was no evidence of the relationship among the electronic characteristi c of the substituents, their displacement on the 6-phenyl ring and the acti vity. Conversely, the displacement of the 2-hydroxyphenyl group in the 4-po sition (4a-e) and of the indol-3-yl group in the 6-position (8h-w) decrease d the anti-inflammatory activity. All derivatives did not show any signific ative antipyretic activity. (C) Elsevier, Paris.