852326-95-5

Upstream product

• 7749-92-0 diethyl 2-formyl-1-phenylethylphosphonate 
• 100-44-7 benzyl chloride 
• 100-51-6 benzyl alcohol 
• 100-52-7 benzaldehyde 
• 33973-22-7 (1-Phenyl-3-butenyl)phosphonsaeure-diethylester 
• 1080-32-6 O,O-diethyl benzylphosphonate 
• 622-33-3 N-benzyloxyamine 
• 884489-13-8 diethyl 3-(benzyloxy)imino-1-phenylpropylphosphonate 
• 884489-14-9 (3-benzyloxyamino-1-phenyl-propyl)-phosphonic acid diethyl ester 
• 2258-42-6 formyl acetic anhydride 

Downstream Products

• 852326-97-7 2,2-dimethyl-propionic acid [3-(benzyloxy-formyl-amino)-1-phenyl-propyl]-(2,2-dimethyl-propionyloxymethoxy)-phosphinoyloxymethyl ester 

Relevant academic research and scientific papers

Antimalarial and structural studies of pyridine-containing inhibitors of 1-deoxyxylulose-5-phosphate reductoisomerase

1-Deoxy-d-xylulose-5-phosphate reductoisomerase (DXR) in the nonmevalonate isoprene biosynthesis pathway is a target for developing antimalarial drugs. Fosmidomycin, a potent DXR inhibitor, showed safety as well as efficacy against Plasmodium falciparum malaria in clinical trials. On the basis of our previous quantitative structure-activity relationship (QSAR) and crystallographic studies, several novel pyridine-containing fosmidomycin derivatives were designed, synthesized, and found to be highly potent inhibitors of P. falciparum DXR (PfDXR) having Ki values of 1.9-13 nM, with the best one being ～11× more active than fosmidomycin. These compounds also potently block the proliferation of multidrug resistant P. falciparum with EC 50 values as low as 170 nM. A 2.3 A? crystal structure of PfDXR in complex with one of the inhibitors is reported, showing that the flexible loop of the protein undergoes conformational changes upon ligand binding and a hydrogen bond and favorable hydrophobic interactions between the pyridine group and the PfDXR account for the enhanced activity.

Synthesis of α-aryl-substituted and conformationally restricted fosmidomycin analogues as promising antimalarials

Fosmidomycin represents a new antimalarial drug that acts by inhibition of 1-deoxy-D-xylulose 5-phosphate reductoisomerase, an essential enzyme of the mevalonate-independent pathway of isoprenoid biosynthesis. This work describes the synthesis of a series

Synthesis and antimalarial activity of chain substituted pivaloyloxymethyl ester analogues of Fosmidomycin and FR900098

Fosmidomycin is a promising antimalarial drug candidate with a unique chemical structure and a novel mode of action. Chain substituted pivaloyloxymethyl ester derivatives of Fosmidomycin and its acetyl analogue FR900098 have been synthesized and their in vitro antimalarial activity versus the Chloroquine sensitive strain 3D7 of Plasmodium falciparum has been determined.