SYNTHESIS AND GCP II INHIBITORY ACTIVITY OF 4[4-(3-BROMOBENZYL)-5-HYDROXYISOXAZOL-3-YL]BENZOIC ACID HETEROCYCLIC ANALOGS

Authors

  • М. Теус Latvian Institute of Organic Synthesis, Riga, LV-1006
  • А. Иргенсонс Latvian Institute of Organic Synthesis, Riga, LV-1006
  • М. Дамброва Latvian Institute of Organic Synthesis, Riga, LV-1006
  • Р. Межапуке Latvian Institute of Organic Synthesis, Riga, LV-1006

DOI:

https://doi.org/10.1007/7343

Keywords:

glutamatecarboxypeptidase II inhibitors, 3-hydroxyisoxazole, 5-hydroxyisoxazole, 5-hydroxypyrazole

Abstract

A method for the synthesis of analogs of glutamate carboxypeptidase II inhibitor 4-[4-(3-bromobenzyl)-5-hydroxyisoxazol-3-yl]benzoic acid – 4-[4-(3-bromobenzyl-5-hydroxypyrazol-3-yl]-benzoic acid and 4-[4-(3-bromobenzyl)-3-hydroxyisoxazol-5-yl]benzoic acid from 4-(2-ethoxycarbonylacetyl)benzoic acid was developed. The GCP II inhibitory activity of all the compounds synthesized was determined. Substitution of the 5-hydroxyisoxazole group by the  5-hydroxypyrazole  group  led toa complete loss of activity, while replacement with the 3-hydroxyylisoxazole  gave  the compound with slightly less inhibitoer activity comparing with the initial compound.

How to Cite
Teus, M.; Jirgensons, A.; Dambrova, M.; Mezhapuke, R.  Chem. Heterocycl. Compd. 2007, 43, 1440. [Khim. Geterotsikl. Soedin. 2007, 1693.]

For this article in the English edition see DOI 10.1007/s10593-007-0222-7


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Published

2023-01-20

Issue

No. 11 (2007)

Section

Original Papers