Substrate analogs for the investigation of deoxyxylulose 5-phosphate reductoisomerase inhibition: synthesis and evaluation
Substrate analogs for the investigation of deoxyxylulose 5-phosphate reductoisomerase inhibition: synthesis and evaluation
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DOI：
10.1016/j.bmcl.2004.08.023
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发表时间：
2004-11-01
影响因子：
2.7
通讯作者：
Proteau, PJ
中科院分区：
文献类型：
--
作者：
Phaosiri, C;Proteau, PJ
合成了5-磷酸脱氧果糖(DXP)类似物，并对其作为重组聚球藻PCC6803 DXP还原异构酶(DXR；EC 1.1.1.267)的替代底物和抑制剂进行了评价。其中5个化合物(1，2-二脱氧-D-苏糖-3-己酮糖-6-磷酸、1-脱氧-L-核酮-5-磷酸、2S，3R-二羟基丁酰胺-4-磷酸、4S-羟基戊烷-2-酮-5-磷酸和3S-羟基戊烷-2-酮-5-磷酸)的竞争性抑制作用比磷霉素弱。第六个化合物，3R，4S-二羟基-5-氧基己基膦酸，作为替代底物，最近报道了与大肠杆菌DXR相同的化合物。(C)2004爱思唯尔有限公司。保留所有权利。
Deoxyxylulose 5-phosphate (DXP) analogs were synthesized and evaluated as alternative substrates and inhibitors of recombinant Synechocystis PCC6803 DXP reductoisomerase (DXR; EC 1.1.1.267). Five of the compounds tested (1,2-dideoxy-D-threo-3-hexulose 6-phosphate, 1-deoxy-L-ribulose 5-phosphate, 2S,3R-dihydroxybutyramide 4-phosphate, 4S-hydroxypentan-2-one 5-phosphate, and 3S-hydroxypentan-2-one 5-phosphate) acted as relatively weak competitive inhibitors when compared to fosmidomycin. A sixth compound, 3R,4S-dihydroxy-5-oxohexylphosphonic acid, served as an alternate substrate, as has recently been reported for the same compound with Escherichia coli DXR. (C) 2004 Elsevier Ltd. All rights reserved.