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Artelinic acid



Artelinic acid
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  ?
PubChem 180423
Chemical data
Formula C23H30O7 
Mol. mass 418.48 g/mol
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.

?

Legal status
Routes  ?

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

  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.
  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.
 
This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Artelinic_acid". A list of authors is available in Wikipedia.
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