(2R,3S)-(+)- and (2S,3R)-(−)-Halofuginone lactate: Synthesis, absolute configuration, and activity against Cryptosporidium parvum
Michael R Linder
1
,
Anja R Heckeroth
1
,
Michael Najdrowski
2
,
A Daugschies
2
,
Dieter Schollmeyer
3
,
Christian Miculka
1
1
Intervet Innovation GmbH, Zur Propstei, 55270 Schwabenheim, Germany.
|
Publication type: Journal Article
Publication date: 2007-08-01
scimago Q2
wos Q2
SJR: 0.472
CiteScore: 5.1
Impact factor: 2.2
ISSN: 0960894X, 14643405
PubMed ID:
17544270
Organic Chemistry
Drug Discovery
Biochemistry
Molecular Biology
Pharmaceutical Science
Clinical Biochemistry
Molecular Medicine
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.
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Total citations:
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Citations from 2024:
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(3.7%)
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GOST
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Linder M. R. et al. (2R,3S)-(+)- and (2S,3R)-(−)-Halofuginone lactate: Synthesis, absolute configuration, and activity against Cryptosporidium parvum // Bioorganic and Medicinal Chemistry Letters. 2007. Vol. 17. No. 15. pp. 4140-4143.
GOST all authors (up to 50)
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Linder M. R., Heckeroth A. R., Najdrowski M., Daugschies A., Schollmeyer D., Miculka C. (2R,3S)-(+)- and (2S,3R)-(−)-Halofuginone lactate: Synthesis, absolute configuration, and activity against Cryptosporidium parvum // Bioorganic and Medicinal Chemistry Letters. 2007. Vol. 17. No. 15. pp. 4140-4143.
Cite this
RIS
Copy
TY - JOUR
DO - 10.1016/j.bmcl.2007.05.053
UR - https://doi.org/10.1016/j.bmcl.2007.05.053
TI - (2R,3S)-(+)- and (2S,3R)-(−)-Halofuginone lactate: Synthesis, absolute configuration, and activity against Cryptosporidium parvum
T2 - Bioorganic and Medicinal Chemistry Letters
AU - Linder, Michael R
AU - Heckeroth, Anja R
AU - Najdrowski, Michael
AU - Daugschies, A
AU - Schollmeyer, Dieter
AU - Miculka, Christian
PY - 2007
DA - 2007/08/01
PB - Elsevier
SP - 4140-4143
IS - 15
VL - 17
PMID - 17544270
SN - 0960-894X
SN - 1464-3405
ER -
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BibTex (up to 50 authors)
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@article{2007_Linder,
author = {Michael R Linder and Anja R Heckeroth and Michael Najdrowski and A Daugschies and Dieter Schollmeyer and Christian Miculka},
title = {(2R,3S)-(+)- and (2S,3R)-(−)-Halofuginone lactate: Synthesis, absolute configuration, and activity against Cryptosporidium parvum},
journal = {Bioorganic and Medicinal Chemistry Letters},
year = {2007},
volume = {17},
publisher = {Elsevier},
month = {aug},
url = {https://doi.org/10.1016/j.bmcl.2007.05.053},
number = {15},
pages = {4140--4143},
doi = {10.1016/j.bmcl.2007.05.053}
}
Cite this
MLA
Copy
Linder, Michael R., et al. “(2R,3S)-(+)- and (2S,3R)-(−)-Halofuginone lactate: Synthesis, absolute configuration, and activity against Cryptosporidium parvum.” Bioorganic and Medicinal Chemistry Letters, vol. 17, no. 15, Aug. 2007, pp. 4140-4143. https://doi.org/10.1016/j.bmcl.2007.05.053.