Interaction of the indole class of vacuolar H(super +)-ATPase inhibitors with lipid bilayers

The study of the interaction of the selective inhibitor of osteoclastic V-ATPase (2Z,4E)-5-(5,6-dichloro-2-indolyl)-2-methoxy-N-(1,2,2,6,6-pentamethylpiperidin-4-yl)-2,4-pentadienamide (SB 242784) with lipid vesicles together with the study of the compound behavior in aqueous solution is reported. The results reveal that with regards to membrane interaction their properties would remain very similar for both molecules, indicating that the differences in inhibition efficiencies are solely a consequence of the molecular recognition processes within the inhibition site in the V-ATPase.