期刊
CHEMICAL & PHARMACEUTICAL BULLETIN
卷 53, 期 6, 页码 653-661出版社
PHARMACEUTICAL SOC JAPAN
DOI: 10.1248/cpb.53.653
关键词
antimalarial agent; beta-carbolinium salt; total synthesis; pi-delocalized lipophilic cationic (DLC) hypothesis; tropical disease; structure-activity relationship
Several beta-carbolines including naturally occurring substances and their corresponding cationic derivatives were synthesized and evaluated for antimalarial (anti plasmodial) activity in vitro and in vivo. A tetracyclic carbolinium salt was elucidated for antileishmanial and antitrypanosomal activities in vitro as well as antiplasmodial activity. Quarternary carbolinium cations showed much higher potencies in vitro than electronically neutral beta-carbolines and a good correlation was observed between pi-delocalized lipophilic cationic (DLC) structure and antimalarial efficacy. beta-Carbolinium compounds exhibit medium suppressive activity in vivo against rodent malaria.
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