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ChemInform Abstract: Phosphonic Analogues of Phenylalanine and Histidine as Strong Inhibitors of Phenylalanine and Histidine Ammonia-Lyases

✍ Scribed by J. ZON

Publisher
John Wiley and Sons
Year
2010
Weight
24 KB
Volume
28
Category
Article
ISSN
0931-7597

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Inhibitors of Phenylalanine Ammonia-Lyas
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## Abstract 2‐Aminoindan‐2‐phosphonic acid (3) was synthesized for the first time both directly from 2‐indanone (7) as well as by alkylation of ethyl diethoxyphosphorylacetate with 1,2‐bis(bromomethyl)benzene (9) via 10–12, respectively. 2‐Hydroxyindan‐2‐phosphonic acid (5) was obtained also from 7

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A series of 5-substituted derivatives of the potent phenylalanine ammonia-lyase (PAL) inhibitor 2aminoindane-2-phosphonic acid (AIP; 2) were synthesized. The AIP analogues 3 ± 7, with additional NO 2 , NH 2 , Me, Br, and OH groups, respectively, were tested as in vitro inhibitors of buckwheat PAL, a