Artelinic acid
From Wikipedia, the free encyclopedia
 |
|
|
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 | |
| ATC code | ? |
| PubChem | |
| 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.
[edit] References
- ^ 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.
- ^ 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:.
- ^ 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:.
