Tetrazole is an effective sn-3 phosphate replacement in substrate analog inhibitors of 14 kDa phospholipase A2

Article abstract of DOI:10.1016/S0960-894X(97)00247-3

A series of substrate analog inhibitors of 14 kDa PLA₂ possessing replacements for the sn-3 phosphate moeity was prepared and evaluated. Tetrazole 26 possessed similar in vitro inhibition potency to phosphate-containing substrate analog inhibitors, but demonstrated superior cell permeability as monitored by LTC₄ release in monocytes.