Artesunate

857

IHS/INP

Antimalarial

TP (Technical Package)

[88495-63-0]

[3 R- (3alpha,5abeta,6beta,8abeta,9alpha,10alpha,12beta,12a R* )]-Butanedioic acid mono(d ecahydro-3,6,9-trimethyl-3,12-epoxy-12 H- pyrano[4,3- j ]-1,2-benzodi oxepin-10-yl) es ter

artesunic acid; dihydroqinghaosu hemisuccinate

C 19 H 28 O 8

384.43

C 59.36%, H 7.34%, O 33.30% .

De rivative of artemisinin, q.v. Prepn: China Cooperative Re search Group on Qinghaosu, J. Tradit. Chinese Med. 2, 9 (1982). Absolute configuration: X.-D. Luo et al., Helv. Chim. Acta 67, 1515 (1984). GC/mass spec. determn.: A. D. Theoha rides et al., Anal. Chem. 60, 115 (1988). Pharmacology: Y. Zhao, J. Trop. Med. Hyg. 88, 391 (1985). Anti malarial activity: W. Peters et al., Ann. Trop. Med. Parasitol. 80, 483 (1986); A. J. Lin et al., J. Med. Chem. 30, 2147 (1987). In hibition of cytochrome oxidase: Y. Zhao et al., J. Nat. Prod. 49, 139 (1986). Toxicology: China Cooperative Research Group on Qinghaosu, J. Tradit. Chinese Med. 2, 31 (1982). Series of articles on chemistry, pharmacology, and antimalarial efficacy: ibid. 3-50.

Fine white crystalline powder

Sodium salt.

C 19 H 27 NaO 8

SM-804

Poor stability in aque ous solutions. LD 50 in mice ( mg/kg ): 520 i.v. ; 475 i.m. (China Cooperative Research Group); also reported as 699 plus or minus 58.5 i.v. (Zhao, 1985)