期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 20, 期 7, 页码 2311-2315出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.01.138
关键词
Orexin receptor; Sleep disorders; Diazepanes
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. (C) 2010 Elsevier Ltd. All rights reserved.
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