Protoberberine alkaloids as antimalarials.

Abstract:

:The protoberberine alkaloids berberine (1), palmatine (2), jatrorrhizine (3), and several berberine derivatives (4-10) were tested for antimalarial activity in vitro against Plasmodium falciparum and in vivo against Plasmodium berghei. The berberine derivatives 4-10 were designed and synthesized to maximize structural diversity within a modest set of compounds. Palmatine (2) and jatrorrhizine (3) were isolated as their chlorides from Enantia chlorantha. None of the protoberberine alkaloids was active in vivo, although compounds 1, 2, 3, 5, and 6 exhibited a potency comparable to that of quinine in vitro.

journal_name

J Med Chem

authors

Vennerstrom JL,Klayman DL

doi

10.1021/jm00401a006

subject

Has Abstract

pub_date

1988-06-01 00:00:00

pages

1084-7

issue

6

eissn

0022-2623

issn

1520-4804

journal_volume

31

pub_type

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