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Artelinic acid

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Artelinic acid
Clinical data
ATC code
  • none
Identifiers
  • 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
CAS Number
PubChem CID
ChemSpider
UNII
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC23H30O7
Molar mass418.486 g·mol−1
3D model (JSmol)
  • O=C(O)c1ccc(cc1)CO[C@H]4O[C@@H]5O[C@@]3(OO[C@]52[C@@H](CC[C@@H](C)[C@@H]2CC3)[C@H]4C)C
  • InChI=1S/C23H30O7/c1-13-4-9-18-14(2)20(26-12-15-5-7-16(8-6-15)19(24)25)27-21-23(18)17(13)10-11-22(3,28-21)29-30-23/h5-8,13-14,17-18,20-21H,4,9-12H2,1-3H3,(H,24,25)/t13-,14-,17+,18+,20+,21-,22-,23-/m1/s1 ☒N
  • Key:UVNHKOOJXSALHN-ILQPJIFQSA-N ☒N
 ☒NcheckY (what is this?)  (verify)

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 artemisinin derivatives arteether and artemether,[2] but is three times more toxic than artesunate.[3] At present,[when?] 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.[when?]

References

[edit]
  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 Organ. 72 (5): 729–35. PMC 2486549. PMID 7955021.
  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 (1): 37–44. doi:10.1016/S0091-3057(00)00309-9. PMID 11113482. S2CID 21246490.
  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.