[Antimalarial activity of deoxoqinghaosu].
Compound 3 (deoxoqinghaosu) and compound 4 (deoxocarbaqinghaosu) were synthesized from arteannuic acid (2). Primary exploration of their antimalarial effect against K173 strain of Plasmodium berghei shows that compound 3 is somewhat more effective than the natural compound--qinghaosu. However, the carba-analogue compound 4 is almost ineffective. The enhanced activity of compound 3 is supposedly ascribed to its higher lipophilicity and, hence, higher affinity for plasmodial membrane. Further studies are in progress.
Ye
B
B
Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences.
Wu
Y L
YL
Li
G F
GF
Jiao
X Q
XQ
D000818:Animals; D000962:Antimalarials; D037621:Artemisinins; D006571:Heterocyclic Compounds / Q000138:chemical synthesis* / Q000494:pharmacology; D008288:Malaria / Q000188:drug therapy; D051379:Mice; D010962:Plasmodium berghei / Q000187:drug effects*; D012717:Sesquiterpenes / Q000138:chemical synthesis* / Q000494:pharmacology
D000962:Antimalarials; D037621:Artemisinins; D006571:Heterocyclic Compounds; D012717:Sesquiterpenes; C063801:deoxoartemisinin; C071629:deoxocarbaqinghaosu