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Title
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Synthesis and evaluation of -halogenated analogues of 3-(acetylhydroxyamino)propylphosphonic acid (FR900098) as antimalarials
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Author
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Abstract
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| 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. |
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Language
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English
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Source (journal)
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Journal of medicinal chemistry. - Washington, D.C., 1963, currens
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Publication
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Washington, D.C.
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2010
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ISSN
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0022-2623
[print]
1520-4804
[online]
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DOI
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10.1021/JM100211E
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Volume/pages
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53
:14
(2010)
, p. 5342-5346
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ISI
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000279787200023
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Full text (Publisher's DOI)
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