| Literature DB >> 11708918 |
P F Jackson1, K L Tays, K M Maclin, Y S Ko, W Li, D Vitharana, T Tsukamoto, D Stoermer, X C Lu, K Wozniak, B S Slusher.
Abstract
A novel series of phosphinic acid based inhibitors of the neuropeptidase NAALADase are described in this work. This series of compounds is the most potent series of inhibitors of the enzyme described to date. In addition, we have shown that these compounds are protective in animal models of neurodegeneration. Compound 34 significantly prevented neurodegeneration in a middle cerebral artery occlusion model of cerebral ischemia. In addition, in the chronic constrictive model of neuropathic pain, compound 34 significantly attenuated the hypersensitivity observed with saline-treated animals. These data suggest that NAALADase inhibition may provide a new approach for the treatment of both neurodegenerative disorders and peripheral neuropathies.Entities:
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Year: 2001 PMID： 11708918 DOI： 10.1021/jm0001774
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446