Synthesis and biological evaluation of two analogues of (S)-α-methyl- 3-carboxyphenylalanine
Two analogues 2, 3 of (S)-α-methyl-3-carboxylphenylalanine 1 were synthesized to test their activity for metabotropic glutamate receptors (mGluRs). Both compounds 2 and 3 were inactive as antagonist for mGluRs, but 2 showed weak agonistic activity for GluR6 in contrast to that reported by Kemp and co-workers.
Ma, Dawei,Ma, Zhaochun,Kozikowski, Alan P.,Pshenichkin, Sergey,Wroblewski, Jarda T.
p. 2447 - 2450
(2007/10/03)
α-METHYL AMINO ACIDS BY CATALYTIC PHASE-TRANSFER ALKYLATIONS
The α-methyl amino acids, α-methyl p-chlorophenylalanine, α-methyl p-tyrosine, α-methyl m-tyrosine and α-methyl DOPA have been prepared in good yields from amino ester hydrochlorides.The key step in the method is the catalytic phase-transfer alkylation of Schiff base derivatives of monoalkyl amino acids.
O'Donnell, Martin J.,LeClef, Brigitte,Rusterholz, David B.,Ghosez, Leon,Antoine, Jean-Pierre,Navarro, Mirtha