In:
ChemMedChem, Wiley, Vol. 3, No. 2 ( 2008-02-15), p. 323-335
Abstract:
The asymmetric synthesis and receptor pharmacology of (1S,2R,3R,5R,6S)‐2‐amino‐3‐Hydroxy‐bicyclo[3.1.0]hexane‐2,6‐dicarboxylic Acid (+)‐ 9 (HYDIA) and a few of its O‐alkylated derivatives are described. The key step of the synthesis utilizes Sharpless’ asymmetric dihydroxylation (AD‐β) for the kinetic resolution of a bicyclic racemic precursor olefin. In contrast to the bicyclic glutamate analogue LY354740, which is a potent and selective agonist for the group II metabotropic glutamate receptors (mGluRs), these new conformationally restricted and also hydroxylated or alkoxylated glutamate analogues are potent and selective antagonists for the group II mGluRs.
Type of Medium:
Online Resource
ISSN:
1860-7179
,
1860-7187
DOI:
10.1002/cmdc.200700226
Language:
English
Publisher:
Wiley
Publication Date:
2008
detail.hit.zdb_id:
2209649-8
SSG:
15,3
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