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

Thomas Verbrugghen UGent, Paul Cos, Louis Maes and Serge Van Calenbergh UGent (2010) JOURNAL OF MEDICINAL CHEMISTRY. 53(14). p.5342-5346
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.
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author
organization
alternative title
Synthesis and evaluation of alpha-halogenated analogues of 3-(acetylhydroxyamino)propylphosphonic acid (FR900098) as antimalarials
year
type
journalArticle (original)
publication status
published
subject
keyword
1-DEOXY-D-XYLULOSE 5-PHOSPHATE REDUCTOISOMERASE, INHIBITORS, SUBSTITUTED FOSMIDOMYCIN ANALOGS, NONMEVALONATE PATHWAY, ISOPRENOID BIOSYNTHESIS, ANTIBACTERIAL, PHOSPHONATES, MALARIA, DRUGS
journal title
JOURNAL OF MEDICINAL CHEMISTRY
J. Med. Chem.
volume
53
issue
14
pages
5342 - 5346
Web of Science type
Article
Web of Science id
000279787200023
JCR category
CHEMISTRY, MEDICINAL
JCR impact factor
5.207 (2010)
JCR rank
3/50 (2010)
JCR quartile
1 (2010)
ISSN
0022-2623
DOI
10.1021/jm100211e
language
English
UGent publication?
yes
classification
A1
copyright statement
I have transferred the copyright for this publication to the publisher
id
1140863
handle
http://hdl.handle.net/1854/LU-1140863
date created
2011-02-07 11:51:04
date last changed
2012-09-05 13:28:57
@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},
  keyword      = {1-DEOXY-D-XYLULOSE 5-PHOSPHATE REDUCTOISOMERASE,INHIBITORS,SUBSTITUTED FOSMIDOMYCIN ANALOGS,NONMEVALONATE PATHWAY,ISOPRENOID BIOSYNTHESIS,ANTIBACTERIAL,PHOSPHONATES,MALARIA,DRUGS},
  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},
}

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, T., 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.