Synthesis of ketone analogues of prolyl and pipecolyl ester FKBP12 ligands

Yong Qian Wu, Douglas E. Wilkinson, David Limburg, Jia He Li, Hansjorg Sauer, Doug Ross, Shi Liang, Dawn Spicer, Heather Valentine, Mike Fuller, Hong Guo, Pam Howorth, Raj Soni, Yi Chen, Joseph P. Steiner, Gregory S. Hamilton

Research output: Contribution to journalArticlepeer-review


The recently discovered small-molecule ligands for the peptidyl and prolyl isomerases (PPIase) of FKBP12 have been shown to possess powerful neuroprotective and neuroregenerative effects. Ketone analogues of the prolyl and pipecolyl esters, which mimic only the FKBP binding domain portion of FK506, are proposed and an efficient synthetic strategy is presented in this report, along with the preliminary results of in vitro and in vivo biological studies.

Original languageEnglish (US)
Pages (from-to)3558-3568
Number of pages11
JournalJournal of medicinal chemistry
Issue number16
StatePublished - Aug 1 2002

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery


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