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Synthesis and evaluation of α-halogenated analogues of 3-(acetylhydroxyamino)propylphosphonic acid (FR900098) as antimalarials

(2010) JOURNAL OF MEDICINAL CHEMISTRY. 53(14). p.5342-5346
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Abstract
Three alpha-halogenated analogues of 3-(acetylhydroxyamino)propylphosphonic acid (FR900098) have been synthesized from diethyl but-3-enylphosphonate using a previously described method for the alpha-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.
Keywords
1-DEOXY-D-XYLULOSE 5-PHOSPHATE REDUCTOISOMERASE, INHIBITORS, SUBSTITUTED FOSMIDOMYCIN ANALOGS, NONMEVALONATE PATHWAY, ISOPRENOID BIOSYNTHESIS, ANTIBACTERIAL, PHOSPHONATES, MALARIA, DRUGS

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Citation

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Chicago
Verbrugghen, Thomas, Paul Cos, Louis Maes, and Serge Van Calenbergh. 2010. “Synthesis and Evaluation of Α-halogenated Analogues of 3-(acetylhydroxyamino)propylphosphonic Acid (FR900098) as Antimalarials.” Journal of Medicinal Chemistry 53 (14): 5342–5346.
APA
Verbrugghen, Thomas, Cos, P., Maes, L., & Van Calenbergh, S. (2010). Synthesis and evaluation of α-halogenated analogues of 3-(acetylhydroxyamino)propylphosphonic acid (FR900098) as antimalarials. JOURNAL OF MEDICINAL CHEMISTRY, 53(14), 5342–5346.
Vancouver
1.
Verbrugghen T, Cos P, Maes L, Van Calenbergh S. Synthesis and evaluation of α-halogenated analogues of 3-(acetylhydroxyamino)propylphosphonic acid (FR900098) as antimalarials. JOURNAL OF MEDICINAL CHEMISTRY. 2010;53(14):5342–6.
MLA
Verbrugghen, Thomas, Paul Cos, Louis Maes, et al. “Synthesis and Evaluation of Α-halogenated Analogues of 3-(acetylhydroxyamino)propylphosphonic Acid (FR900098) as Antimalarials.” JOURNAL OF MEDICINAL CHEMISTRY 53.14 (2010): 5342–5346. Print.
@article{1140863,
  abstract     = {Three alpha-halogenated analogues of 3-(acetylhydroxyamino)propylphosphonic acid (FR900098) have been synthesized from diethyl but-3-enylphosphonate using a previously described method for the alpha-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.},
  author       = {Verbrugghen, Thomas and Cos, Paul and Maes, Louis and Van Calenbergh, Serge},
  issn         = {0022-2623},
  journal      = {JOURNAL OF MEDICINAL CHEMISTRY},
  language     = {eng},
  number       = {14},
  pages        = {5342--5346},
  title        = {Synthesis and evaluation of \ensuremath{\alpha}-halogenated analogues of 3-(acetylhydroxyamino)propylphosphonic acid (FR900098) as antimalarials},
  url          = {http://dx.doi.org/10.1021/jm100211e},
  volume       = {53},
  year         = {2010},
}

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