Cardiff University | Prifysgol Caerdydd ORCA
Online Research @ Cardiff 
WelshClear Cookie - decide language by browser settings

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., 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

Full text not available from this repository.

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: 13 Nov 2017 15:11
URI: http://orca.cf.ac.uk/id/eprint/105889

Citation Data

Cited 11 times in Scopus. View in Scopus. Powered By Scopus® Data

Actions (repository staff only)

Edit Item Edit Item