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 Chemjournal_title
Journal of medicinal chemistryauthors
Vennerstrom JL,Klayman DLdoi
10.1021/jm00401a006subject
Has Abstractpub_date
1988-06-01 00:00:00pages
1084-7issue
6eissn
0022-2623issn
1520-4804journal_volume
31pub_type
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