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Arteether, a new antimalarial drug: synthesis and antimalarial properties
Abstract
Arteether (6) has been prepared from dihydroquinghaosu (3) by etherification with ethanol in the presence of Lewis acid and separated from its chromatographically slower moving alpha-dihydroqinghaosu ethyl ether (7). The absolute stereochemistry at C-12 has been determined by 1H NMR data (J11,12, NOESY). Ethyl ethers 6 and 7 showed potent in vitro inhibition of Plasmodium falciparum, and both compounds were highly potent antimalarials in mice infected with a drug-sensitive strain of Plasmodium berghei. Crystalline arteether (6) and its oily epimer 7 were 2-3 times more potent schizontocides than quinghaosu (1), but deoxy compounds 8, 9, and 11 were 100-300 times less potent in vitro than their corresponding peroxy precursors. Pharmacological studies have shown arteether(6) to have antimalarial activity in animals comparable to artesunate (2) and artemether (4), both of which are fast-acting blood schizontocides in humans. Arteether (6) has now been chosen for a clinical evaluation in high-risk malaria patients.
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Citations
Cited by
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Meshnick, S. R. (2002) · International Journal for Parasitology · doi:10.1016/s0020-7519(02)00194-7 · Cited by 720
The modification of natural products for medical use
Guo, Z. (2017) · Acta Pharmaceutica Sinica B · doi:10.1016/j.apsb.2016.06.003 · Cited by 328
Iron-dependent free radical generation from the antimalarial agent artemisinin (qinghaosu)
Meshnick, S. R., Yang, Y. Z., Lima, V, Kuypers, F., Kamchonwongpaisan, S., & Yuthavong, Y. (1993) · Antimicrobial Agents and Chemotherapy · doi:10.1128/aac.37.5.1108 · Cited by 327
Artemisinin and the antimalarial endoperoxides: from herbal remedy to targeted chemotherapy
Meshnick, S. R., Taylor, T. E., & Kamchonwongpaisan, S. (1996) · Microbiological Reviews · doi:10.1128/mmbr.60.2.301-315.1996 · Cited by 710
“This was confirmed by scientists at the Walter Reed Army Institute of Research (13).”
BackgroundInfluentialde Vries, P. J., & Dien, T. K. (1996) · Drugs · doi:10.2165/00003495-199652060-00004 · Cited by 277
Metadata
- Authors
- Brossi, A., Venugopalan, B., Dominguez Gerpe, L., Yeh, H. J. C., Flippen-Anderson, J. L., Buchs, P., Luo, X. D., Milhous, W., & Peters, W.
- Venue
- Journal of Medicinal Chemistry
- Publisher
- American Chemical Society (ACS)
- Published
- 1988-03
- Volume
- 31
- Issue
- 3
- Pages
- 645-650
- ISSN
- 0022-2623 (ISSN-L)
- 1520-4804
- OpenAlex
- W2090081368
- Cited by
- 320
- References
- 0
- FWCI
- 15.32
- Type
- journal article
- Language
- en
- Open access
- closed
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- Brossi, A., Venugopalan, B., Dominguez Gerpe, L., Yeh, H. J. C., Flippen-Anderson, J. L., Buchs, P., Luo, X. D., Milhous, W., & Peters, W. (1988). Arteether, a new antimalarial drug: synthesis and antimalarial properties. Journal of Medicinal Chemistry. https://doi.org/10.1021/jm00398a026
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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
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