| Abstract
| - Amino acid ester prodrugs of 2-bromo-5,6-dichloro-1-(β-d-ribofuranosyl)benzimidazole (BDCRB)were synthesized and evaluated for their affinity for hPEPT1, an intestinal oligopeptidetransporter. Assays of competitive inhibition of [3H]glycylsarcosine (Gly-Sar) uptake in HeLa/hPEPT1 cells by the amino acid ester prodrugs of BDCRB suggested their 2- to 4-fold higheraffinity for hPEPT1 compared to BDCRB. Further, promoieties with hydrophobic side chainsand l-configuration were preferred by the hPEPT1 transporter.
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