Bioorganic & Medicinal Chemistry Letters 2006-01-01

Synthesis and preliminary biological evaluation of (2S,1'R,2'S)- and (2S,1'S,2'R)-2-(2'-phosphonocyclopropyl)glycines, two novel conformationally constrained l-AP4 analogues.

Laura Amori, Michaela Serpi, Maura Marinozzi, Gabriele Costantino, Monica Gavilan Diaz, Mette Brunsgaard Hermit, Christian Thomsen, Roberto Pellicciari

Index: Bioorg. Med. Chem. Lett. 16 , 196-9, (2006)

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Abstract

Two novel constrained l-AP4 analogues, (2S,1'R,2'S)- and (2S,1'S,2'R)-2-(2'-phosphonocyclopropyl)glycines (7) and (8), were synthesized and evaluated as mGluR ligands. Compound 7 showed to be a group III mGluRs agonist with micromolar activity.