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.