Synthesis and preliminary biological evaluation of (2S,1′R,2′S)-and (2S,1S,2′R)-2-(2′-phosphonocyclopropyl)glycines, two novel conformationally constrained L-AP4 analogues

被引：21

作者：

Amori, L

Serpi, M

Marinozzi, M

Costantino, G

Diaz, MG

Hermit, MB

Thomsen, C

Pellicciari, R

机构：

[1] Univ Perugia, Dipartimento Chim & Tecnol Farm, I-06123 Perugia, Italy

[2] H Lundbeck & Co AS, DK-2500 Copenhagen, Denmark

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 01期

关键词：

D O I：

10.1016/j.bmcl.2005.09.014

中图分类号：

R914 [药物化学];

学科分类号：

100701 [药物化学];

摘要：

Two novel constrained L-AP4 analogues, (2S,1'R,2'S)- and (2S,1'S,2R)-2-(2'-phosphonocyclopropyl)glycines (7) and (8), were synthesized and evaluated as mGluR ligands. Compound 7 showed to be a group III mGluRs agonist with micromolar activity. (c) 2005 Elsevier Ltd. All rights reserved.

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页码：196 / 199

页数：4

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