Synthesis, SARs, and pharmacological characterization of 2-amino-3 or 6-fluorobicyclo [3.1. 0] hexane-2, 6-dicarboxylic acid derivatives as potent, selective, and …
(+)-2-Aminobicyclo [3.1. 0] hexane-2, 6-dicarboxylic acid (4, LY354740), a highly selective and orally active group II metabotropic glutamate receptor (mGluR) agonist, has increased interest in the study of group II mGluRs. Our interest focused on a conformationally constrained form of compound 4, because it appeared that the rigid form resulted in not only selectivity for group II mGluR but was orally active. Therefore, we introduced a fluorine ...
