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THE SYNTHESIS OF NOVEL 2,4,6-TRISUBSTITUTED 1,3,5-TRIAZINES: A SEARCH FOR POTENTIAL MURF ENZYME INHIBITORS

  作者 SOSIC IZIDOR; STEFANE BOGDAN; KOVAC ANDREJA; TURK SAMO; BLANOT DIDIER; GOBEC STANISLAV  
  选自 期刊  Heterocycles;  卷期  2010年81-1;  页码  91-115  
  关联知识点  
 

[摘要]A series of new 2,4,6-trisubstituted 1,3,5-triazines, possessing a variety of substituents (-OH, -SH, -OMe, -Cl, -HNR, -SR and amino acid moieties), were synthesized and evaluated for the inhibition of the bacterial peptidoglycan biosynthesis enzyme MurF. Ethoxycarbonyl isothiocyanate successfully reacted with a variety of amidines, enabling an approach to 6-substituted-4-thioxo-1,3,5-triazin-2-ones. Also, a representative set of 2-thio-, 2-amino-, and 2-oxo-substituted 1,3,5-triazines was synthesized by the SNAr reaction, employing 2,4,6-trichloro-1,3,5-triazine and 2-chloro-4,6-dimethoxy-1,3,5-triazine as the starting materials. One compound displayed notable inhibitory activity against MurF from Escherichia coli.

 
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