Michelle Armstrong
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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.

Lavieri R, Scott SA, Lewis JA, Selvy PE, Armstrong MD, Alex Brown H, Lindsley CW
Bioorg Med Chem Lett. 2009 19 (8): 2240-3

PMID: 19299128 · PMCID: PMC3800051 · DOI:10.1016/j.bmcl.2009.02.125

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.

MeSH Terms (6)

Dose-Response Relationship, Drug Drug Design Enzyme Inhibitors Isoenzymes Phospholipase D Structure-Activity Relationship

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