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Synthesis and antiprotozoal activities of simplified analogs of naphthylisoquinoline alkaloids.

Abstract：

:The naphthylisoquinoline alkaloids (NIQs) represent a class of natural products with manifold activities against various tropical diseases. They are isolated from rare and difficult-to-cultivate tropical plants. In order to find novel, more easily accessible analogs and to study structure-activity relationships, a variety of simplified analogs were produced, which bear the functional groups typical of the NIQs, but avoid the synthetically difficult elements of chirality, stereogenic centers and rotationally hindered axes. Their syntheses and activities against Plasmodium falciparum, Trypanosoma cruzi, and Leishmania donovani are described and compared with those of the natural NIQs. Remarkably, quite good activities were found for naphthalene-devoid halogenated isoquinolinic analogs.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Bringmann G,Brun R,Kaiser M,Neumann S

doi

10.1016/j.ejmech.2007.03.003

subject

Has Abstract

pub_date

2008-01-01 00:00:00

pages

32-42

issue

1

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(07)00125-0

journal_volume

43

pub_type

杂志文章

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