四氢噻吩和四氢呋喃的合成及其作为黑皮质素-4受体配体的衍生物研究。
Syntheses of tetrahydrothiophenes and tetrahydrofurans and studies of their derivatives as melanocortin-4 receptor ligands.
作者信息
Tran Joe A, Chen Caroline W, Tucci Fabio C, Jiang Wanlong, Fleck Beth A, Chen Chen
机构信息
Department of Medicinal Chemistry, Neurocrine Biosciences, Inc., 12790 El Camino Real, San Diego, CA 92130, USA.
出版信息
Bioorg Med Chem Lett. 2008 Feb 1;18(3):1124-30. doi: 10.1016/j.bmcl.2007.11.128. Epub 2007 Dec 5.
Piperazinebenzylamine derivatives from trans-4-(4-chlorophenyl)tetrahydrothiophene-3-carboxylic acid 6 and its S-oxide 7 and sulfone 8, and the tetrahydrofuran 9 and its two regioisomers 11 and 13 were synthesized and studied for their binding affinities at the human melanocortin-4 receptor. These five-membered ring constrained compounds possessed similar or lower potency compared to the acyclic analogs.
合成了反式-4-(4-氯苯基)四氢噻吩-3-羧酸6及其S-氧化物7和砜8的哌嗪苄胺衍生物，以及四氢呋喃9及其两种区域异构体11和13，并研究了它们与人促黑素皮质素-4受体的结合亲和力。与无环类似物相比，这些五元环受限化合物具有相似或更低的效力。
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