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 …

…, T Kumagai, K Sakagami, R Yoshikawa…

Index: Nakazato; Kumagai; Sakagami; Yoshikawa; Suzuki; Chaki; Ito; Taguchi; Nakanishi; Okuyama Journal of Medicinal Chemistry, 2000 , vol. 43, # 25 p. 4893 - 4909

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Citation Number: 107

Abstract

(+)-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 ...