Artelinic acid

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Artelinic acid
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Systematic (IUPAC) name
4-[(3R,5aS,6R,8aS,9R,10S,12R,12aR)-decahydro-
3,6,9-trimethyl-3,12-epoxy-12H-pyrano[4,3-j]-1,2-
benzodioxepin-10-yl]oxy]methylbenzoic acid
Identifiers
CAS Number 120020-26-0
ATC code none
PubChem CID 180423
Chemical data
Formula C23H30O7
Molar mass 418.48 g/mol[[Script error: No such module "String".]]
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Artelinic acid (or its salt, artelinate) is an experimental drug that is being investigated as a treatment for malaria.[1] It is a semi-synthetic derivative of the natural compound artemisinin. Artelinic acid has a lower rate of neurotoxicity than the related artemisin derivatives arteether and artemether,[2] but is three times more toxic than artesunate.[3] At present, artelinic acid seems unlikely to enter routine clinical use, because it offers no clear benefits over the artemesinins already available (artesunate and artemether). Artelinic acid has not yet been evaluated for use in humans.

References

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  1. Bustos MD, Gay F, Diquet B. (1994). "In-vitro tests on Philippine isolates of Plasmodium falciparum against four standard antimalarials and four qinghaosu derivatives". Bull World Health Org. 72: 729–35. 
  2. Genovese RF, Newman DB, Brewer TG (2000). "Behavioural and neural toxicity of the artemisinin antimalarial, arteether, but not artesunate and artelinate, in rats". Pharmacol Biochem Behav. 67: 37–44. doi:10.1016/S0091-3057(00)00309-9. 
  3. Li Q, Xie LH, Johnson TO; et al. (2007). "Toxicity exaluation of artesunate and artelinate in Plasmodium berghei-infected and uninfected rats". Trans R Soc Trop Med Hyg Z. 101 (2): 104–12. doi:10.1016/j.trstmh.2006.04.010. PMID 16860356.