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Abstract

The reduction of the peptide bond of enalapril results in a compound, enamipril, which does not show polarized and saturable transport from the mucosal to the serosal side of the intestinal tissue. Also because the transport of enamipril cannot be inhibited by cephalexin, the analogue with the reduced peptide bond is no longer a substrate for the intestinal small-peptide carrier. Therefore, it can be concluded that the carbonyl group is an essential structural requirement for transport by the small-peptide carrier. In contrast, the interaction with the small-peptide carrier is still present, shown by the inhibition of the fluxes of amoxycillin. Reduction of the peptide bond of enalapril resulted in a new substrate for the P-glycoprotein efflux pump.

Effect of Sodium Diclofenac on Serum and Tissue Concentration of Amoxicillin and on Staphylococcal Infection

“…26) Peptide transporters were not usually associated with diclofenac absorption. However, other drugs, such as amiloride 27) and enalapril, 28) having a high affinity for peptide transporters, caused a significant decrease in amoxicillin concentration.…”

Multiple-Ligand-Based Virtual Screening: Methods and Applications of the MTree Approach

“…This pharmacological family encompasses ACE inhibitors, among other compounds, which suggests true ACE inhibitory activity for some hits. One molecule, DR9902034 (enamipril), has no activity label, while it corresponds to enalapril (see Figure ) with a reduced alanine carbonyl group …”