作为褪黑素结合位点MT3上新配体的苯并呋喃衍生物的设计与合成。
Design and synthesis of benzofuranic derivatives as new ligands at the melatonin-binding site MT3.
作者信息
Ettaoussi Mohamed, Péres Basile, Klupsch Fréderique, Delagrange Philippe, Boutin Jean-A, Renard Pierre, Caignard Daniel-H, Chavatte Philippe, Berthelot Pascal, Lesieur Daniel, Yous Saïd
机构信息
Laboratoire de Chimie Thérapeutique (EA 1043), Faculté des Sciences Pharmaceutiques et Biologiques, Université de Lille, 3, rue du professeur Laguesse, 2, BP 83, 59006 Lille Cedex, France.
出版信息
Bioorg Med Chem. 2008 May 1;16(9):4954-62. doi: 10.1016/j.bmc.2008.03.036. Epub 2008 Mar 17.
Benzofuranic analogues of MCA-NAT (5-methoxycarbonylamino-N-acetyltryptamine) have been synthesized and evaluated as melatonin receptor ligands. Introduction of a methoxycarbonylamino substituent in the C-5 position of the benzofurane nucleus obtains MT(3) selective ligands. This selectivity can be modulated with suitable variations of the C-5 position and the acyl group on the C-3 side chain.
已合成了褪黑素受体激动剂N-乙酰-5-甲氧基羰基氨基色胺（MCA-NAT）的苯并呋喃类似物，并将其作为褪黑素受体配体进行了评估。在苯并呋喃核的C-5位引入甲氧基羰基氨基取代基可得到MT(3)选择性配体。这种选择性可通过C-5位和C-3侧链上酰基的适当变化来调节。
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