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).

Bioorganic & medicinal chemistry letters (2007-03-14)

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

PMID17350839

摘要

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.