Synthesis and evaluation of \alpha$ -halogenated analogues of 3-(acetylhydroxyamino)propylphosphonic acid (FR900098) as antimalarials
| Autor: | Louis Maes, Serge Van Calenbergh, Thomas Verbrugghen, Paul Cos |
|---|---|
| Jazyk: | angličtina |
| Rok vydání: | 2010 |
| Předmět: |
inorganic chemicals
PHOSPHONATES Plasmodium berghei Stereochemistry ISOPRENOID BIOSYNTHESIS Plasmodium falciparum Antimalarials Mice Structure-Activity Relationship MALARIA 1-deoxy-D-xylulose 5-phosphate reductoisomerase Fosfomycin In vivo Drug Discovery parasitic diseases ANTIBACTERIAL DRUGS Animals Structure–activity relationship Potency NONMEVALONATE PATHWAY biology Chemistry Pharmacology. Therapy biology.organism_classification In vitro Malaria Isoprenoid biosynthesis Acute Disease Molecular Medicine 1-DEOXY-D-XYLULOSE 5-PHOSPHATE REDUCTOISOMERASE INHIBITORS SUBSTITUTED FOSMIDOMYCIN ANALOGS |
| Zdroj: | Journal of medicinal chemistry JOURNAL OF MEDICINAL CHEMISTRY |
| ISSN: | 0022-2623 |
| Popis: | Three α-halogenated analogues of 3-(acetylhydroxyamino)propylphosphonic acid (FR900098) have been synthesized from diethyl but-3-enylphosphonate using a previously described method for the α-halogenation of alkylphosphonates. These analogues were evaluated for antimalarial potential in vitro against Plasmodium falciparum and in vivo in the P. berghei mouse model. All three analogues showed higher in vitro and/or in vivo potency than the reference compounds. |
| Databáze: | OpenAIRE |
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