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Azaterphenyl diamidines as antileishmanial agents.

Abstract：

:Eighteen diamidino azaterphenyls and analogues were evaluated as anti-leishmanials; nine of the compounds gave IC50 values less than 1 microM, five exhibited values less than 0.40 microM, and two gave values less than 0.10 microM in a Leishmania donovani axenic amastigote assay. The activity of the diamidines strongly depends on the ring N-atom location relative to the amidine groups and correlates with DNA affinity. Transmission electron microscopy studies showed a dramatic dilation of the mitochondrion and evidence of disintegration of the kinetoplast of the amastigotes.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Hu L,Arafa RK,Ismail MA,Wenzler T,Brun R,Munde M,Wilson WD,Nzimiro S,Samyesudhas S,Werbovetz KA,Boykin DW

doi

10.1016/j.bmcl.2007.10.091

subject

Has Abstract

pub_date

2008-01-01 00:00:00

pages

247-51

issue

1

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(07)01273-5

journal_volume

18

pub_type

杂志文章

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