73226-73-0

Usage

Chemical Properties

Pale Brown Solid

Biochem/physiol Actions

1-deoxy-D-xylulose 5-phosphate reductoisomerase (DXR) is an enzyme involved in the first step in the nonmevalonate pathway for isoprenoid biosynthesis in Gram-negative, Gram-positive bacteria, plants, and the parasite causing the most virulent form of malaria, Plasmodium falciparum (Mammals produce isoprenoids via the mevalonate pathway). Inhibiton of the enzyme provides alternative to traditional antimalaria therapy. FR-900098 is twice more effective than fosmidomycin against various strains of P. falciparum in vitro and the closely related P. vinckei in mice.

Upstream product

• 60-29-7 diethyl ether 
• 66508-11-0 3-(N-hydroxyamino)-propylphosphonic acid 
• 71-36-3 butan-1-ol 
• 581106-28-7 [3-[acetyl(phenylmethoxy)amino]propyl]phosphonic acid diethyl ester 
• 1003599-68-5 dibenzyl {3-[acetyl(benzyloxy)amino]propyl}phosphonate 
• 108-24-7 acetic anhydride 
• 66508-32-5 3-(N-acetyl-N-hydroxyamino)propylphosphonic acid 

Downstream Products

• 66508-11-0 3-(N-hydroxyamino)-propylphosphonic acid 

Relevant academic research and scientific papers

Synthesis and antiplasmodial activity of novel fosmidomycin derivatives and conjugates with artemisinin and aminochloroquinoline

Malaria, despite many efforts, remains among the most problematic infectious diseases worldwide, mainly due to the development of drug resistance by Plasmodium falciparum. The antibiotic fosmidomycin (FSM) is also known for its antimalarial activity by targeting the nonmevalonate isoprenoid synthesis pathway, which is essential for the malaria parasites but is absent in mammalians. In this study, we synthesized and evaluated against the chloroquine-resistant P. falciparum FcB1/Colombia strain, a series of FSM analogs, derivatives, and conjugates with other antimalarial agents, such as artemisinin (ART) and aminochloroquinoline (ACQ). The biological evaluation revealed four new compounds with higher antimalarial activity than FSM: two FSM-ACQ derivatives and two FSM-ART conjugates, with 3.5–5.4 and 41.5–23.1 times more potent activities than FSM, respectively.

Synthesis of antimalarial compounds fosmidomycin and FR900098 through N- or P-alkylation reactions

Two straightforward and convenient routes for the synthesis of the antimalarial agents FR900098 and fosmidomycin are described. In the key steps N- or P-alkylation reactions are used. The best overall yields of FR900098 and fosmidomycin in 15 mmol scale a

Synthesis of the antimalarial drug FR900098 utilizing the nitroso-ene reaction

The antimalarial drug FR900098 was prepared from diethyl allylphosphonate involving the nitroso-ene reaction with nitrosocarbonyl methane as the key step followed by hydrogenation and dealkylation. The utilization of dibenzyl allylphosphonate as the start

Use of organophosphorus compounds for the therapeutic and prophylactic treatment of infections

Use of organophosphorus compounds of general Formula (I) for the therapeutic and prophylactic treatment of infections in humans and animals caused by viruses, fungi and parasites.

Herbicidal hydroxyamino phosphonic acids and derivatives

Compounds having the formula STR1 wherein R1 is a acyl, R2 is hydrogen, lower alkyl, ar(lower)alkyl or acyl, and A is lower alkylene, lower alkenylene or hydroxy(lower)alkylene, or an agronomically-acceptable salt or ester thereof, a

Hydroxyaminohydrocarbonphosphonic acids

New hydroxyaminohydrocarbonphosphonic acid derivatives of the formula: STR1 wherein R1 is hydrogen or acyl, R2 is hydrogen, lower alkyl, ar(lower)alkyl or acyl, and A is lower alkylene, lower alkenylene or hydroxy(lower)alkylene, or