254737-42-3Relevant articles and documents
Synthesis and biological evaluation of thiol-based inhibitors of glutamate carboxypeptidase II: Discovery of an orally active GCP II inhibitor
Majer, Pavel,Jackson, Paul F.,Delahanty, Greg,Grella, Brian S.,Ko, Yao-Sen,Li, Weixing,Liu, Qun,Maclin, Keith M.,Poláková, Jana,Shaffer, Kathryn A.,Stoermer, Doris,Vitharana, Dilrukshi,Yanjun Wang, Eric,Zakrzewski, Anthony,Rojas, Camilo,Slusher, Barbara S.,Wozniak, Krystyna M.,Burak, Eric,Limsakun, Tharin,Tsukamoto, Takashi
, p. 1989 - 1996 (2007/10/03)
A series of 2-(thioalkyl)pentanedioic acids were synthesized and evaluated as inhibitors of glutamate carboxypeptidase II (GCP II, EC 3.4.17.21). The inhibitory potency of these thiol-based compounds against GCP II was found to be dependent on the number of methylene units between the thiol group and pentanedioic acid. A comparison of the SAR of the thiol-based inhibitors to that of the phosphonate-based inhibitors provides insight into the role of each of the two zinc-binding groups in GCP II inhibition. The most potent thiol-based inhibitor, 2-(3-mercaptopropyl)pentanedioic acid (IC50 = 90 nM), was found to be orally bioavailable in rats and exhibited efficacy in an animal model of neuropathic pain following oral administration.
Methods for treating anxiety, anxiety disorders and memory impairment using naaladase inhibitors
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, (2008/06/13)
The present invention relates to methods of using NAALADase inhibitors for treating glutamate-mediated diseases, disorders and conditions selected from the group consisting of anxiety, anxiety disorders and memory impairment.
