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Synthesis and antimalarial activity of calothrixins A and B, and their N-alkyl derivatives.
Matsumoto, Kohji; Choshi, Tominari; Hourai, Mai; Zamami, Yoshito; Sasaki, Kenji; Abe, Takumi; Ishikura, Minoru; Hatae, Noriyuki; Iwamura, Tatsunori; Tohyama, Shigeo; Nobuhiro, Junko; Hibino, Satoshi.
Bioorg Med Chem Lett ; 22(14): 4762-4, 2012 Jul 15.
Article in English | MEDLINE | ID: mdl-22727670

ABSTRACT

We synthesized calothrixin B using our developed biomimetic method and derived N-alkyl-calothrixins A and B. The in vitro antimalarial activity of the calothrixin derivatives, including calothrixins A and B, against the Plasmodium falciparum FCR-3 strain was evaluated. All test compounds exhibited antimalarial activity over a concentration range of 6.4×10(-6)-1.2×10(-7) M.


Subject(s)
Antimalarials/chemical synthesis , Indole Alkaloids/chemistry , Alkylation , Antimalarials/pharmacology , Indole Alkaloids/pharmacology , Molecular Structure , Plasmodium falciparum/drug effects , Structure-Activity Relationship
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