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(2R,3S)-(+)- and (2S,3R)-(-)-Halofuginone lactate: synthesis, absolute configuration, and activity against Cryptosporidium parvum.

作者信息

Linder Michael R, Heckeroth Anja R, Najdrowski Michael, Daugschies Arwid, Schollmeyer Dieter, Miculka Christian

机构信息

Intervet Innovation GmbH, Zur Propstei, 55270 Schwabenheim, Germany.

出版信息

Bioorg Med Chem Lett. 2007 Aug 1;17(15):4140-3. doi: 10.1016/j.bmcl.2007.05.053. Epub 2007 May 21.

DOI:10.1016/j.bmcl.2007.05.053
PMID:17544270
Abstract

The trans-enantiomers of the commercially important anti-protozoal compound Halofuginone have been prepared and characterized, and the absolute configuration was assigned by X-ray crystallography. The activity of both enantiomers against Cryptosporidium parvum was determined in vitro and related to acute toxicity in vivo. It was shown that both the activity and the toxicity are properties of the (2R,3S)-enantiomer. We conclude that with respect to broadening the therapeutic window there is no advantage in application of one enantiomer over the application of the racemic mixture in the treatment of C. parvum infections.

摘要

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