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

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

Affiliation

  • 1 Department of Medicinal Chemistry, Neurocrine Biosciences Inc., 12790 El Camino Real, San Diego, CA 92130, USA. mrowbottom@neurocrine.com
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.

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