2. Academic Validation
  3. Design and synthesis of isoform-selective phospholipase D (PLD) inhibitors. Part II. Identification of the 1,3,8-triazaspiro[4,5]decan-4-one privileged structure that engenders PLD2 selectivity

Design and synthesis of isoform-selective phospholipase D (PLD) inhibitors. Part II. Identification of the 1,3,8-triazaspiro[4,5]decan-4-one privileged structure that engenders PLD2 selectivity

  • Bioorg Med Chem Lett. 2009 Apr 15;19(8):2240-3. doi: 10.1016/j.bmcl.2009.02.125.
Robert Lavieri 1,  Sarah A Scott,  Jana A Lewis,  Paige E Selvy,  Michelle D Armstrong,  H Alex Brown,  Craig W Lindsley
Affiliations

Affiliation

  • 1 Department of Pharmacology, Vanderbilt University, Nashville, TN 37232, USA.
PMID: 19299128 DOI: 10.1016/j.bmcl.2009.02.125
Abstract

This Letter describes the synthesis and structure-activity relationships (SAR) of isoform-selective PLD inhibitors. By virtue of the installation of a 1,3,8-triazaspiro[4,5]decan-4-one privileged structure, PLD inhibitors with nanomolar potency and an unprecedented 40-fold selectivity for PLD2 over PLD1 were developed. Interestingly, SAR for this diverged from our earlier efforts, and dual PLD1/2 inhibitors were also discovered within this series.

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