发明名称 |
AROMATISCHE VERBINDUNGEN ALS ALDOLASE INHIBITOREN |
摘要 |
<p>Formyl-hydroxy-naphthyl-phosphate (or phosphate mimetic) compounds (I), in which the aldehyde and phenol groups are attached to adjacent C-atoms of one ring and the phosphate (or phosphate mimetic) group is attached to a C-atom of the other ring, are new. Hydroxy-naphthaldehyde derivatives of formula (I) are new. [Image] R : phosphate group or phosphate-mimetic group, selected from (i) enzyme-labile protecting groups allowing (I) to pass passively through cell and/or parasite membranes, such that a phosphate group (or stable analog) is formed when (I) is inside the cell or parasite or (ii) stable phosphate group analogs such that (I) is protected against spontaneous and/or enzymatic dephosphorylation; the aldehyde and phenol groups are attached to adjacent C-atoms of one ring and R is attached to a carbon atom of the other ring; (I) is optionally further ring-substituted by at least one hydrophobic group (Q) for improving the overall hydrophobicity of (I). An independent claim is included for the preparation of (I). ACTIVITY : Cytostatic; Antiparasitic. MECHANISM OF ACTION : Class I aldolase inhibitor; glycolysis inhibitor. 5-Formyl-6-hydroxy-2-naphthyl-phosphate (Ia) had an overall inhibition constant (K* i) of 40 20 nM for rabbit muscle aldolase.</p> |
申请公布号 |
AT398625(T) |
申请公布日期 |
2008.07.15 |
申请号 |
AT20040767508T |
申请日期 |
2004.06.29 |
申请人 |
UNIVERSITE PAUL SABATIER TOULOUSE III;CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS);VALORISATION-RECHERCHE, SOCIETE EN COMMANDITE |
发明人 |
DAX, CHANTAL;BLONSKI, CASIMIR;AZEMA, LAURENT;SYGUSCH, JURGEN |
分类号 |
C07F9/12 |
主分类号 |
C07F9/12 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
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