Abstract
The design of prodrugs suitable for transport by the dipeptide transporter can be a useful strategy for improving the absorption of small polar drugs which exhibit very poor bioavailability.A series of dipeptides (thirty two dipeptide compounds), in which the C-terminal residue is proline or a proline ester, has been synthesized. The inhibitory effect of these dipeptides on the uptake of the dipeptide Gly-Pro by a Caco-2 cell line has been determined by using tritium labeled substrates.
The results suggest the dipeptide with proline benzyl ester and Glutamic acid benzyl ester has a good inhibitory activity.
Date of Award | 2001 |
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Original language | English |
Awarding Institution |
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Keywords
- Design
- dipeptides
- probes
- gastrointestinal
- transport
- system