Synthesis and Biological Activities of Conformationally Restricted Cyclopentenyl-Glutamate Analogues
摘要:
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 (EC50 18 muM) and mGlu2 (EC50 45 muM) receptors.
Synthesis and Biological Activities of Conformationally Restricted Cyclopentenyl-Glutamate Analogues
摘要:
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 (EC50 18 muM) and mGlu2 (EC50 45 muM) receptors.
Synthesis and Biological Activities of Conformationally Restricted Cyclopentenyl-Glutamate Analogues
作者:Alison T. Ung、Karl Schafer、Karl B. Lindsay、Stephen G. Pyne、Kitti Amornraksa、Ria Wouters、Ilse Van der Linden、Ilse Biesmans、Anne S. J. Lesage、Brian W. Skelton、Allan H. White
DOI:10.1021/jo010864i
日期:2002.1.1
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 (EC50 18 muM) and mGlu2 (EC50 45 muM) receptors.