ω -Phosphinyl-α -Amino Acids: Synthesis, and Development towards Use as Therapeutic Agents

Author(s): Nick J. Wardle , S. W. Annie Bligh , Harry R. Hudson .

Journal Name: Current Organic Chemistry

Volume 11 , Issue 18 , 2007

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Abstract:

Literature publications (up to September 2006) concerning the synthesis of ω-phosphinyl-α-amino acids and their development towards use as therapeutic agents are reviewed. General and asymmetric methodologies for the preparation of straight-chain examples are described, including AP3-7 modulators of glutamate-responsive excitatory amino acid (EAA) receptors (i.e. ionotropic NMDA-, and metabotropic GrpIII mGlu-receptors), and the glutamate synthetase inhibitor phosphinothricin. Focusing primarily on the development of methods for introducing phosphonate and aminocarboxylate functions to the appropriate scaffold, approaches to conformationally constrained ω-phosphinyl-α-amino acids are also investigated, along with their relevance to the development of therapeutic regimens towards neurodegenerative disorders.

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Article Details

VOLUME: 11
ISSUE: 18
Year: 2007
Page: [1635 - 1651]
Pages: 17
DOI: 10.2174/138527207783221200
Price: $58

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