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ID: ALA1156317

Journal: Bioorg Med Chem Lett

Title: Design and synthesis of conformationally constrained N,N-disubstituted 1,4-diazepanes as potent orexin receptor antagonists.

Authors: Coleman PJ, Schreier JD, McGaughey GB, Bogusky MJ, Cox CD, Hartman GD, Ball RG, Harrell CM, Reiss DR, Prueksaritanont T, Winrow CJ, Renger JJ.

Abstract: Orexins are neuropeptides that regulate wakefulness and arousal. Small molecule antagonists of orexin receptors may provide a novel therapy for the treatment of insomnia and other sleep disorders. In this Letter we describe the design and synthesis of conformationally constrained N,N-disubstituted 1,4-diazepanes as orexin receptor antagonists. The design of these constrained analogs was guided by an understanding of the preferred solution and solid state conformation of the diazepane central ring.

CiteXplore: 20207138

DOI: 10.1016/j.bmcl.2010.01.138