磷霉素的N-酰化磺酰胺类似物对1-脱氧-D-木酮糖-5-磷酸还原异构酶没有任何抑制活性。
N-acylated sulfonamide congeners of fosmidomycin lack any inhibitory activity against DXR.
作者信息
Gadakh Bharat, Pouyez Jenny, Wouters Johan, Venkatesham Akkaladevi, Cos Paul, Van Aerschot Arthur
机构信息
Medicinal Chemistry, Rega Institute for Medical Research, KU Leuven, Minderbroedersstraat 10, 3000 Leuven, Belgium.
Department of Chemistry, University of Namur, Rue de Bruxelles 61, Namur B-5000, Belgium.
出版信息
Bioorg Med Chem Lett. 2015 Apr 1;25(7):1577-9. doi: 10.1016/j.bmcl.2015.02.006. Epub 2015 Feb 12.
The antibiotic fosmidomycin (3a) is an inhibitor of the non-mevalonate pathway for isoprenoid biosynthesis. Four analogues in which an acylated sulfonamide group is substituting for its phosphonate moiety have been synthesized in a fruitless effort to preserve one negative charge in order to increase the accompanying affinity for 1-deoxy-d-xylulose 5-phosphate reductoisomerase (DXR), the fosmidomycin target enzyme.
抗生素磷霉素（3a）是类异戊二烯生物合成非甲羟戊酸途径的抑制剂。为了保留一个负电荷以增强对磷霉素的靶酶1-脱氧-D-木酮糖-5-磷酸还原异构酶（DXR）的亲和力，已合成了四种用酰化磺酰胺基团取代其膦酸酯部分的类似物，但未取得成功。
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