title: Synthesis and antimalarial efficacy of aza-fused rhodacyanines in vitro and in the P. berghei mouse model.
abstract: Several aza-fused rhodacyanines were synthesized and assessed for their in vitro and in vivo antimalarial activities against Plasmodium falciparum K1 and P. berghei. All synthetic compounds showed strong selective antimalarial in vitro activity. Class II azarhodacyanines, 3, consisting of four heterocyclic units, were found to display good parasitemia suppression and low acute toxicity in vivo. Among them, 3c appeared to be the most effective at a dose of 20-25 mg kg(-1) day(-1) (ip).
authors.affiliation: Department of Organic Chemistry, Graduate School of Pharmaceutical Sciences, Tohoku University, Aobayama, Sendai 980-8578, Japan. kay-t@mail.pharm.tohoku.ac.jp
authors.forename: Kiyosei
authors.initials: K
authors.lastname: Takasu
authors.forename: Khanitha
authors.initials: K
authors.lastname: Pudhom
authors.forename: Marcel
authors.initials: M
authors.lastname: Kaiser
authors.forename: Reto
authors.initials: R
authors.lastname: Brun
authors.forename: Masataka
authors.initials: M
authors.lastname: Ihara
mesh_terms: D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D001372:Aza Compounds / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D002460:Cell Line; D004351:Drug Resistance; D008288:Malaria / Q000188:drug therapy*; D051379:Mice; D010962:Plasmodium berghei / Q000187:drug effects*; D010963:Plasmodium falciparum / Q000187:drug effects; D011726:Pyridinium Compounds / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D013844:Thiazoles / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity
chemical_list: D000962:Antimalarials; D001372:Aza Compounds; D011726:Pyridinium Compounds; D013844:Thiazoles; C481079:rhodacyanine