Abstract
A new series of 2-(5-methoxy-2-methyl-1
-indol-3-yl)-
′-[(
)-(substituted phenyl) methylidene] acetohydrazide derivatives (
⁻
) were synthesized and evaluated for their anti-inflammatory activity, analgesic activity, ulcerogenic activity, lipid peroxidation, ulcer index and cyclooxygenase expression activities. All the synthesized compounds were in good agreement with spectral and elemental analysis. Three synthesized compounds (
,
and
) have shown significant anti-inflammatory activity as compared to the reference drug indomethacin. Compound
was further tested for ulcerogenic index and cyclooxygenase (COX) expression activity. It was selectively inhibiting COX-2 expression and providing the gastric sparing activity. Docking studies have revealed the potential of these compounds to bind with COX-2 enzyme. Compound
formed a hydrogen bond between OH of Tyr 355 and NH₂ of Arg 120 with carbonyl group and this hydrogen bond was similar to that formed by indomethacin. This study provides insight for compound
, as a new lead compound as anti-inflammatory agent and selective COX-2 inhibitor.