Laboratory for Medicinal Chemistry, Ghent University, Ottergemsesteenweg 460, B-9000 Ghent, Belgium.
Laboratory for Microbiology, Parasitology and Hygiene, University of Antwerp, Universiteitsplein 1 (S7), B-2610 Wilrijk, Belgium.
Bioorg Med Chem Lett. 2019 May 1;29(9):1051-1053. doi: 10.1016/j.bmcl.2019.03.008. Epub 2019 Mar 7.
A series of N-alkoxy analogs of a l-leucine ethyl ester phosphonodiamidate prodrug of a fosmidomycin surrogate were synthesized and investigated for their ability to inhibit in vitro growth of P. falciparum and M. tuberculosis. These compounds originate by merging a previously reported successful phosphonate derivatisation with favorable modifications of the hydroxamate moiety. None of the synthesized compounds showed enhanced activity against either P. falciparum or M. tuberculosis in comparison with the parent free hydroxamate analog.
合成了一系列 N-烷氧基类似物作为磷霉素替代物的 l-亮氨酸乙酯膦酸二酰胺前药，并研究了它们抑制疟原虫和结核分枝杆菌体外生长的能力。这些化合物来源于对先前报道的成功的膦酸衍生物进行合并，并对异羟肟酸部分进行了有利的修饰。与母体游离异羟肟酸类似物相比，合成的化合物对疟原虫或结核分枝杆菌均没有表现出增强的活性。
