Novel δ2-isoxazolines as group II phospholipase A2 inhibitors

The synthesized imidazolyl substituted delta(2)-isoxazolines were subjected to Phospholipase A(2) (PLA(2)) enzyme inhibitory activity against snake venom source and their structure-activity relationship with respect to different groups attached to this moiety is reported for the first time. The crystal structure of the compound 2-butyl-5-chloro-3H-imidazolyl-4-carbaldehyde oxime 2, an intermediate for the construction of isoxazolines is reported. These compounds exerted a significant PLA2 enzyme inhibitory activity against group II PLA2. The in vivo activity on mice of selected compounds 3bI and 3bIV shows the comparable anti-inflammatory activity with the known standard ursolic acid. (C) 2004 Elsevier Ltd. All rights reserved.