构象受限的环戊烯基 - 谷氨酸类似物的合成及生物活性
Synthesis and biological activities of conformationally restricted cyclopentenyl-glutamate analogues.
作者信息
Ung Alison T, Schafer Karl, Lindsay Karl B, Pyne Stephen G, Amornraksa Kitti, Wouters Ria, Van der Linden Ilse, Biesmans Ilse, Lesage Anne S J, Skelton Brian W, White Allan H
机构信息
Department of Chemistry, University of Wollongong, Wollongong, NSW, 2522, Australia.
出版信息
J Org Chem. 2002 Jan 11;67(1):227-33. doi: 10.1021/jo010864i.
An efficient method for preparing conformationally restricted cyclopentenyl-glutamate analogues in a regioselective and diastereoselective manner has been developed using a formal [3 + 2] cycloaddition reaction of dehydroamino acids. Methods for preparing optically active versions of these compounds have also been devised. Of these compounds, (S)-2 is an agonist at the mGlu5 (EC(50) 18 microM) and mGlu2 (EC(50) 45 microM) receptors.
已开发出一种利用脱氢氨基酸的形式[3 + 2]环加成反应以区域选择性和非对映选择性方式制备构象受限环戊烯基谷氨酸类似物的有效方法。还设计了制备这些化合物光学活性形式的方法。在这些化合物中，(S)-2是mGlu5（EC(50) 18 microM）和mGlu2（EC(50) 45 microM）受体的激动剂。
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