In the previous paper, several benzyloxybenzaldehyde isomers were synthesized and found to have significant inhibitory activity toward neutrophil superoxide formation. Among them, 2-benzyloxybenzaldehyde (CCY1a) was the most promising one, which was identified as an novel adenyl cyclase inhibitor. In this present work, CCY1a was selected as lead compound, a series of CCY1a derivatives was synthesized and their inhibitory effects on neutrophil superoxide anion formation was evaluated. The structure-activity relationships in this series were also examined. All of the derivatives of (2E)-3-{2-[(substituted benzyl)oxy]-substituted phenyl}acrylaldehyde showed potent activity. Among them, (2E)-3-[2-(benzyloxy)-5-methoxyphenyl]acrylaldehyde was the most promising one which could provide a novel structural prototype for anti-inflammatory agents.
