2001
DOI: 10.1016/s0960-894x(01)00075-0
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Diaryl ester prodrugs of fR900098 with improved in vivo antimalarial activity

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Cited by 91 publications
(56 citation statements)
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“…10 Also, the phosphonate moiety has been altered to produce prodrugs with improved oral bioavailability. 11,12,13 Interestingly, modifications addressing the three carbon spacer are scarce. The objective of this work was to synthesize a series of fosmidomycin or FR900098 analogues containing a phenyl moiety in the α-position.…”
Section: [Figure 1]mentioning
confidence: 99%
“…10 Also, the phosphonate moiety has been altered to produce prodrugs with improved oral bioavailability. 11,12,13 Interestingly, modifications addressing the three carbon spacer are scarce. The objective of this work was to synthesize a series of fosmidomycin or FR900098 analogues containing a phenyl moiety in the α-position.…”
Section: [Figure 1]mentioning
confidence: 99%
“…These include modifications of the phosphonate group that yield phosphonate prodrugs expected to enhance oral availability. 22,23 Different acyl group substituents have also been prepared, as well as modifications of the hydroxamate group and of the three-carbon spacer (see, for example, references [24][25][26] and other work cited therein).…”
Section: Introductionmentioning
confidence: 99%
“…Furthermore, this study encourages the development of new inhibitors of the nonmevalonate pathway with increased bioavailability and enhanced antimalarial activity. A derivative of fosmidomycin, FR900098, and a prodrug of this compound have been shown to be more effective than fosmidomycin in the mouse model (5,11). Since fosmidomycin represents a simple molecule, which can be synthesized from cheap raw materials, cost-efficient, large-scale production seems possible.…”
Section: Discussionmentioning
confidence: 99%