Bioorganic & Medicinal Chemistry Letters 2007-04-15

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

Martin W Rowbottom, 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

Index: Bioorg. Med. Chem. Lett. 17 , 2171-2178, (2007)

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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.