Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 18, Issue 1, Pages 247-251Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2007.10.091
Keywords
Leishmania; diamidines; azaterphenyl; DNA binding; Suzuki coupling
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Eighteen diamidino azaterphenyls and analogues were evaluated as anti-leishmanials; nine of the compounds gave IC50 values less than 1 mu M, five exhibited values less than 0.40 mu M, and two gave values less than 0.10 mu M 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. (C) 2007 Elsevier Ltd. All rights reserved.
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