Synthesis and antimalarial activity of calothrixins A and B, and their N-alkyl derivatives.
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.
Graduate School of Pharmacy & Pharmaceutical Sciences, and Faculty of Pharmacy and Pharmaceutical Sciences, Fukuyama University, Fukuyama, Hiroshima 729-0292, Japan.
Kohji
K
Matsumoto
Tominari
T
Choshi
Mai
M
Hourai
Yoshito
Y
Zamami
Kenji
K
Sasaki
Takumi
T
Abe
Minoru
M
Ishikura
Noriyuki
N
Hatae
Tatsunori
T
Iwamura
Shigeo
S
Tohyama
Junko
J
Nobuhiro
Satoshi
S
Hibino
D000478:Alkylation; D000962:Antimalarials / Q000138:chemical synthesis* / Q000494:pharmacology; D026121:Indole Alkaloids / Q000737:chemistry* / Q000494:pharmacology; D015394:Molecular Structure; D010963:Plasmodium falciparum / Q000187:drug effects; D013329:Structure-Activity Relationship
D000962:Antimalarials; D026121:Indole Alkaloids; C418328:calothrixin A; C418327:calothrixin B