Synthesis and structure-activity relationships of spirohydantoin-derived small-molecule antagonists of the melanin-concentrating hormone receptor-1 (MCH-R1)

  • Bioorg Med Chem Lett. 2007 Apr 15;17(8):2171-8. doi: 10.1016/j.bmcl.2007.01.104.
Martin W Rowbottom  1 ,  Troy D Vickers ,  Junko Tamiya ,  Mingzhu Zhang ,  Brian Dyck ,  Jonathan Grey ,  David Schwarz ,  Christopher E Heise ,  Michael Hedrick ,  Jenny Wen ,  Hui Tang ,  Hua Wang ,  Andrew Fisher ,  Anna Aparicio ,  John Saunders ,  Val S Goodfellow
Affiliations
  • 1. Department of Medicinal Chemistry, Neurocrine Biosciences Inc., 12790 El Camino Real, San Diego, CA 92130, USA. [email protected]
PMID: 17350839 DOI: 10.1016/j.bmcl.2007.01.104
Abstract

The design, synthesis, and SAR of a series of substituted spirohydantoins are described. Optimization of an in-house screening hit gave compounds that exhibited potent binding affinity and functional activity at MCH-R1.

Products