Optimization of halopemide for phospholipase D2 inhibition

  • Bioorg Med Chem Lett. 2007 Apr 15;17(8):2310-1. doi: 10.1016/j.bmcl.2007.01.059.
Lauren Monovich  1 ,  Benjamin Mugrage ,  Elizabeth Quadros ,  Karen Toscano ,  Ruben Tommasi ,  Stacey LaVoie ,  Eugene Liu ,  Zhengming Du ,  Daniel LaSala ,  William Boyar ,  Paul Steed
Affiliations
  • 1. Novartis Institutes for BioMedical Research, 100 Technology Square, Cambridge, MA 02139, USA. [email protected]
PMID: 17317170 DOI: 10.1016/j.bmcl.2007.01.059
Abstract

Halopemide, which was identified by HTS to inhibit Phospholipase D2 (PLD2), provided the basis for an exploratory effort to identify potent inhibitors of PLD2 for use as inflammatory mediators. Parallel synthesis and purification were utilized to rapidly identify orally available amide analogs derived from indole 2-carboxylic acids with superior potency versus PLD2.

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