摘要 |
Amino acid ester, dipeptide, and tripeptide ester derivatives of bioactive agents are provided wherein said parent agents are substrates effluxed by the P-gp transporter. The derivatives are useful in treating the same condition as the bioactve agent. Also disclosed is a method for preparing a bioactive agent for targeted delivery by nutrient or peptide transporters comprising linking the agent to one or more groups of the formula -X-Y<SUB>(n)</SUB>-Z<SUB>(n')</SUB>-Z<SUP>'</SUP><SUB>(n'')</SUB>-R; wherein each X, Y, Z, and Z' is independently Met, Val, Thr, Tyr, Trp, Ser, Ala or Gly; R is independently H or an amino-protecting group; and each n, n', or n'' is independently 0 or 1. |