31066-00-9Relevant academic research and scientific papers
4-Alkoxybenzamidines as new potent phospholipase A2 inhibitors
Aitdafoun, Mina,Mounier, Carine,Heymans, Francoise,Binisti, Carine,Cassian, Bon,Godfroid, Jean-Jacques
, p. 737 - 742 (2007/10/03)
A series of 4-alkoxybenzamidines was synthesized, varying the number of carbons of the alkyl chain, and their potency as phospholipase A2 (PLA2) inhibitors was evaluated. The relationship between their capacity to inhibit PLA2 activity and their lipophilicity was examined. The optimum of the inhibitory effect against two extracellular PLA2s from rabbit platelets and bovine pancreas was observed with compounds bearing an alkyl chain of 12 and 14 carbons. These 4-dodecyl and tetradecyloxybenzamidines inhibited bovine pancreatic and rabbit platelet lysate PLA2s with IC50 values of 3 μM and 5-5.8 μM, respectively. The mechanism of inhibition was of the competitive type. In addition, 4-tetradecyloxybenzamidine was shown to exert an anti-inflammatory effect in vivo on the carrageenan-induced rat paw oedema. These results show that 4-tetradecyloxybenzamidine will serve as an interesting tool to investigate the physiological role of mammalian-secreted PLA2, both in vitro and in vivo.
