The design and synthesis of inhibitors of pantothenate synthetase

被引:43
作者
Tuck, Kellie L.
Saldanha, S. Adrian
Birch, Louise M.
Smith, Alison G.
Abell, Chris
机构
[1] Univ Cambridge, Chem Lab, Cambridge CB2 1EW, England
[2] Dept Plant Sci, Cambridge CB2 3EA, England
关键词
D O I
10.1039/b609482a
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
Pantothenate synthetase catalyses the ATP-dependent condensation of D-pantoate and beta-alanine to form pantothenate. Ten analogues of the reaction intermediate pantoyl adenylate, in which the phosphodiester is replaced by either an ester or sulfamoyl group, were designed as potential inhibitors of the enzyme. The esters were all modest competitive inhibitors, the sulfamoyls were more potent, consistent with their closer structural similarity to the pantoyl adenylate intermediate.
引用
收藏
页码:3598 / 3610
页数:13
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