Microwave-Enhanced α-Arylation of a Protected Glycine in Water:Evaluation of 3-Phenylglycine Derivatives as Inhibitors of the Tuberculosis Enzyme, Glutamine Synthetase

Author(s): Olof Lagerlund, Luke R. Odell, Sherry L. Mowbray, Mikael T. Nilsson, Wojciech W. Krajewski, Anneli Nordqvist, Anders Karlen, Mats Larhed.

Journal Name: Combinatorial Chemistry & High Throughput Screening
Accelerated Technologies for Biotechnology, Bioassays, Medicinal Chemistry and Natural Products Research

Volume 10 , Issue 9 , 2007

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A microwave-enhanced, palladium-catalyzed protocol for the α-arylation of a protected glycine in neat water is described. This reaction proceeds rapidly, under non-inert conditions, to afford a range of phenylglycine derivatives in moderate to good yields. Based on this α-arylation, a number of aryl L-methionine-SR-sulfoximine (MSO) analogues were prepared and evaluated for their Mycobacterium tuberculosis glutamine synthetase (TB-GS) inhibitory activity.

Keywords: Arylation, glutamine synthetase, microwave, palladium, tuberculosis, water

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Article Details

Year: 2007
Page: [783 - 789]
Pages: 7
DOI: 10.2174/138620707783018478
Price: $58

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