Synthesis and GCP II inhibitory activity of 4[4-(3-bromobenzyl)-5-hydroxyisoxazol-3-yl]benzoic acid heterocyclic analogs |
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Authors: | M Teus A Jirgensons M Dambrova R Mezhapuke |
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Institution: | (1) Latvian Institute of Organic Synthesis, Riga, LV-1006, Latvia |
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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.
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Translated from Khimiya Geteritsiklicheskikh Soedinenii, No. 11, 1693–1697, November, 2007. |
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Keywords: | glutamatecarboxypeptidase II inhibitors 3-hydroxyisoxazole 5-hydroxyisoxazole 5-hydroxypyrazole |
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