Synthesis and structure-activity relationship of N-acyl-Gly-, N-acyl-Sar- and N-blocked-boroPro inhibitors of FAP, DPP4, and POP.

@article{Tran2007SynthesisAS,
  title={Synthesis and structure-activity relationship of N-acyl-Gly-, N-acyl-Sar- and N-blocked-boroPro inhibitors of FAP, DPP4, and POP.},
  author={Thuy H Tran and Clifford L Quan and Conrad Yap Edosada and Mark Mayeda and Christian Wiesmann and Dan Sutherlin and Beni B. Wolf},
  journal={Bioorganic & medicinal chemistry letters},
  year={2007},
  volume={17 5},
  pages={1438-42}
}
The structure-activity relationship of various N-acyl-Gly-, N-acyl-Sar-, and N-blocked-boroPro derivatives against three prolyl peptidases was explored. Several N-acyl-Gly- and N-blocked-boroPro compounds showed low nanomolar inhibitory activity against fibroblast activation protein (FAP) and prolyl oligopeptidase (POP) and selectivity against dipeptidyl peptidase-4 (DPP4). N-Acyl-Sar-boroPro analogs retained selectivity against DPP4 and potent POP inhibitory activity but displayed decreased… CONTINUE READING