Protoberberine Alkaloids as Antimalarials

Jonathan L Vennerstrom, Daniel L. Klayman

Research output: Contribution to journalArticle

97 Citations (Scopus)

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.

Original languageEnglish (US)
Pages (from-to)1084-1087
Number of pages4
JournalJournal of Medicinal Chemistry
Volume31
Issue number6
DOIs
StatePublished - Feb 1 1988

Fingerprint

Berberine
Antimalarials
Alkaloids
Berberine Alkaloids
Plasmodium berghei
Quinine
Plasmodium falciparum
Chlorides
jatrorrhizine
protoberberine
In Vitro Techniques
palmatine

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

Cite this

Protoberberine Alkaloids as Antimalarials. / Vennerstrom, Jonathan L; Klayman, Daniel L.

In: Journal of Medicinal Chemistry, Vol. 31, No. 6, 01.02.1988, p. 1084-1087.

Research output: Contribution to journalArticle

Vennerstrom, Jonathan L ; Klayman, Daniel L. / Protoberberine Alkaloids as Antimalarials. In: Journal of Medicinal Chemistry. 1988 ; Vol. 31, No. 6. pp. 1084-1087.
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