Synthesis and antimalarial efficacy of aza-fused rhodacyanines in vitro and in the P. berghei mouse model.
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).
Takasu
Kiyosei
K
Department of Organic Chemistry, Graduate School of Pharmaceutical Sciences, Tohoku University, Aobayama, Sendai 980-8578, Japan. kay-t@mail.pharm.tohoku.ac.jp
Pudhom
Khanitha
K
Kaiser
Marcel
M
Brun
Reto
R
Ihara
Masataka
M
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
D000962:Antimalarials; D001372:Aza Compounds; D011726:Pyridinium Compounds; D013844:Thiazoles; C481079:rhodacyanine