The discovery and synthesis of JNJ 31020028, a small molecule antagonist of the Neuropeptide Y Y2 receptor

Swanson, Devin M., Wong, Victoria D., Jablonowski, Jill A., Shah, Chandra, Rudolph, Dale A., Dvorak, Curt A., Seierstad, Mark, Dvorak, Lisa K., Morton, Kirsten, Nepomuceno, Diane, Atack, John R. ORCID: https://orcid.org/0000-0002-3410-791X, Bonaventure, Pascal, Lovenberg, Timothy W. and Carruthers, Nicholas I. 2011. The discovery and synthesis of JNJ 31020028, a small molecule antagonist of the Neuropeptide Y Y2 receptor. Bioorganic and Medicinal Chemistry Letters 21 (18) , pp. 5552-5556. 10.1016/j.bmcl.2011.06.136

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Abstract

A series of small molecules based on a chemotype identified from our compound collection were synthesized and tested for binding affinity (IC50) at the human Neuropeptide Y Y2 receptor (NPY Y2). Six of the 23 analogs tested possessed an NPY Y2 IC50 ⩽ 15 nM. One member of this series, JNJ 31020028, is a selective, high affinity, receptor antagonist existing as a racemic mixture. As such a synthetic route to the desired enantiomer was designed starting from commercially available (S)-(+)-mandelic acid.

Item Type:	Article
Date Type:	Publication
Status:	Published
Schools:	Biosciences
Publisher:	Elsevier
ISSN:	0960-894X
Date of Acceptance:	20 June 2011
Last Modified:	03 Nov 2022 09:45
URI:	https://orca.cardiff.ac.uk/id/eprint/105889

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