| Autor: |
V. Slavíková, K. Slavík, V. Zlkán, J. Volejníková, M. Semonský |
| Rok vydání: |
1969 |
| Předmět: |
|
| Zdroj: |
Biochemical Pharmacology. 18:1455-1461 |
| ISSN: |
0006-2952 |
| DOI: |
10.1016/0006-2952(69)90259-7 |
| Popis: |
Several derivatives and analogues of β-4-methoxybenzoyl-β-bromoacrylic acid (MBBA) have been tested as inhibitors of tetrahydrofolate formylase from pigeon liver and the effect of structural changes on the inhibitory activity has been studied. The inhibitory effect is dependent on a halogen atom in the β-position of the acrylate moiety adjoining the double bond and further by the free carboxyl of the acrylate moiety. Every change in this area leads to complete loss of the inhibitory activity. Substitution of the 4 position in the aromatic nucleus by an alkyi or alkoxy group enhances the inhibitory effect, the length of the aliphatic chain being without considerable effect. Substitution by an acetamido group suppresses the effect considerably. The methylation or methoxylation of the aromatic nucleus in the 2, 3 and 6 positions considerably diminishes the inhibitory activity, but it does not eliminate completely the inhibitory effect. Preincubation of MBBA with tetrahydrofolate formylase does not influence the inhibitory effect; the dialysis of the enzyme-MBBA mixture (either preincubated or not) leads to complete recovery of tetrahydrofolate formylase activity. The, inhibition of the enzyme by MBBA and similar substances seems to be completely reversible. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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