942631-72-3Relevant academic research and scientific papers
ORGANOPHOSPHORIC DERIVATIVES USEFUL AS ANTI-PARASITIC AGENTS
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Page/Page column 60-61, (2008/06/13)
The present invention relates to novel phosphonic acid compounds having the structural formula (I): wherein: (a) R is a group of 1 to 5 substituents independently selected from the group consisting of fluoro, chloro, bromo, C1-4 alkoxy, C1
Divergent strategy for the synthesis of α-aryl-substituted fosmidomycin analogues
Devreux, Vincent,Wiesner, Jochen,Jomaa, Hassan,Rozenski, Jef,Van Der Eycken, Johan,Van Calenbergh, Serge
, p. 3783 - 3789 (2008/02/01)
(Chemical Equation Presented) Fosmidomycin is the first representative of a new class of antimalarial drugs acting through inhibition of 1-deoxy-D-xylulose 5-phosphate (DOXP) reductoisomerase (DXR), an essential enzyme in the non-mevalonate pathway for the synthesis of isoprenoids. This work describes a divergent strategy for the synthesis of a series of α-aryl-substituted fosmidomycin analogues, featuring a palladium-catalyzed Stille coupling as the key step. An α-(4-cyanophenyl)fosmidomycin analogue emerged as the most potent analogue in the present series. Its antimalarial activity clearly surpasses that of the reference compound fosmidomycin.
Synthesis and evaluation of α,β-unsaturated α-aryl-substituted fosmidomycin analogues as DXR inhibitors
Devreux, Vincent,Wiesner, Jochen,Jomaa, Hassan,Van der Eycken, Johan,Van Calenbergh, Serge
, p. 4920 - 4923 (2008/02/11)
Fosmidomycin, which acts through inhibition of 1-deoxy-d-xylulose phosphate reductoisomerase (DXR) in the non-mevalonate pathway, represents a valuable recent addition to the armamentarium against uncomplicated malaria. In this paper, we describe the synt
