2. Academic Validation
  3. Discovery and structure-activity relationship of 1,3-cyclohexyl amide derivatives as novel mGluR5 negative allosteric modulators

Discovery and structure-activity relationship of 1,3-cyclohexyl amide derivatives as novel mGluR5 negative allosteric modulators

  • Bioorg Med Chem Lett. 2013 Mar 1;23(5):1398-406. doi: 10.1016/j.bmcl.2012.12.078.
Hao Zhou 1,  Sidney W Topiol,  Michel Grenon,  Hermogenes N Jimenez,  Michelle A Uberti,  Daniel G Smith,  Robbin M Brodbeck,  Gamini Chandrasena,  Henrik Pedersen,  Jens Christian Madsen,  Darío Doller,  Guiying Li
Affiliations

Affiliation

  • 1 Discovery Chemistry & DMPK, Lundbeck Research USA, 215 College Road, Paramus, NJ 07652, USA.
PMID: 23357634 DOI: 10.1016/j.bmcl.2012.12.078
Abstract

A novel series of trans-1,3-cyclohexyl diamides was discovered and characterized as mGluR5 negative allosteric modulators (NAMs) lacking an alkyne moiety. Conformational constraint of one of the amide bonds in the diamide template led to a spirooxazoline template. A representative compound (24d) showed good in vitro potency, high CNS penetration and, upon subcutaneous dosing, demonstrated efficacy in the mouse marble burying test, generally used as indicative of potential anxiolytic activity.

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