Identification of GCP II Inhibitors Based on 4-Arylmethyl-3-(4-carboxyphenyl)-5-hydroxyisoxazole Scaffold

Letters in Drug Design & Discovery 2009
Marina Teus, Aigars Jirgensons, Maija Dambrova, Rudolfs Mezapuke, Chris Graham Parsons, Wojciech Danysz

Screening of a non-ionizable compound library and hit optimization studies has resulted in a series of compounds based on a 4-arylmethyl-3-(4-carboxyphenyl)-5-hydroxyisoxazole scaffold with GCP II inhibitory activity in the low micromolar range.

Keywords
glutamate carboxypeptidase II, glutamate, 5-hydroxyisoxazole, lipophilicity, synthesis
DOI
10.2174/157018009787158544

Teus, M., Jirgensons, A., Dambrova, M., Mezapuke, R., Parsons, C., Danysz, W. Identification of GCP II Inhibitors Based on 4-Arylmethyl-3-(4-carboxyphenyl)-5-hydroxyisoxazole Scaffold. Letters in Drug Design & Discovery, 2009, Vol.6, No.1, pp.29-32. ISSN 1570-1808. Available from: doi:10.2174/157018009787158544

Publication language
English (en)