4.5 Article

Optimization of halopemide for phospholipase D2 inhibition

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 17, Issue 8, Pages 2310-2311

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2007.01.059

Keywords

halopemide; phospholipase D; inhibitor

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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. (c) 2007 Elsevier Ltd. All rights reserved.

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