title: New semisynthetic quassinoids with in vivo antimalarial activity.
abstract: On the basis of a comparative analysis for stability in mouse serum between 15-O-acetylbruceolide and bruceolide 15-methyl carbonate, several 3,15-dialkyl carbonates of bruceolide were synthesized and their in vitro antimalarial activity was assessed. Methyl, ethyl, and isopropyl carbonates with pronounced in vitro activity were further evaluated for in vivo antimalarial potency. Both the methyl and ethyl carbonates significantly increased the life span of mice as compared with 3,15-di-O-accetylbruceolide and chloroquine.
authors.affiliation: Graduate School of Pharmaceutical Sciences, Osaka University, 1-6 Yamada-oka, Suita, Osaka 565-0871, Japan.
authors.forename: Nobutoshi
authors.initials: N
authors.lastname: Murakami
authors.forename: Masanori
authors.initials: M
authors.lastname: Sugimoto
authors.forename: Motoyuki
authors.initials: M
authors.lastname: Kawanishi
authors.forename: Satoru
authors.initials: S
authors.lastname: Tamura
authors.forename: Hye-Sook
authors.initials: HS
authors.lastname: Kim
authors.forename: Khurshida
authors.initials: K
authors.lastname: Begum
authors.forename: Yusuke
authors.initials: Y
authors.lastname: Wataya
authors.forename: Motomasa
authors.initials: M
authors.lastname: Kobayashi
mesh_terms: D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D004355:Drug Stability; D008288:Malaria / Q000188:drug therapy; D051379:Mice; D010962:Plasmodium berghei; D010963:Plasmodium falciparum / Q000187:drug effects*; D036702:Quassins / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured
chemical_list: D000962:Antimalarials; D036702:Quassins