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This compound (1-(phenylmethyl)-2-piperizinyl benzimidazole or lerisetron) is shown in figure 1and is a potent 5-HT 3 R antagonist.
Functional groups on this compound capable of forming interactions with the receptor are the distal amino group, a benzimidazole and a benzyl group in the N1 position of the benzimidazole.
While Lerisetron contains no carbonyl group, the second nitrogen contained in the benzimidazole heterocycle could act as bioisostere of this functional group [ 22 ] .
W89 is shown interacting with the aromatic benzimidazole group of lerisetron although the precise position of W89 relative to this group is not known.
Since the benzimidazole group is common to all three compounds it is the most likely point of interaction.
Our data does not support an interaction of this amino acid with either the N-benzyl or benzimidazole portions of lerisetron.
Therefore, blocking the final process in hydrogen ion secretion reduces acid secretion and this is the mechanism of action of the substituted benzimidazole agents known as proton pump inhibitors (PPI).
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