Design and synthesis of potential dual NK₁/NK₃ receptor antagonists

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• 作者：Stephen Hanessian ; Vincent Babonneau ; Nicolas Boyer ; Clotilde Mannoury la Cour ; Mark J. Millan ; Guillaume De Nanteuil
• 关键词：Schizophrenia ; Neurokinin receptors ; Peptidomimetic ; NK1/NK3 receptor antagonists
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：15 January, 2014
• 年：2014
• 卷：24
• 期：2
• 页码：510-514
• 全文大小：1199 K

文摘

The tachykinin NK₁ and NK₃ receptors are a novel drug target for schizophrenia in order to treat not only the positive and cognitive symptoms, but also the associated co-morbid depression and sleep disturbances associated with the disease. A novel class of peptidomimetic derivatives based on a versatile phenylglycine central core was synthesized and tested in vitro as dual NK₁/NK₃ receptor antagonists. From this series emerged compounds with good NK₁ receptor affinity, although only modest dual NK₁/NK₃ receptor affinity was observed with one of these analogs.