| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1376918 | Bioorganic & Medicinal Chemistry Letters | 2008 | 5 Pages |
Abstract
Eighteen diamidino azaterphenyls and analogues were evaluated as anti-leishmanials; nine of the compounds gave IC50 values less than 1 μM, five exhibited values less than 0.40 μM, and two gave values less than 0.10 μM 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.
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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Laixing Hu, Reem K. Arafa, Mohamed A. Ismail, Tanja Wenzler, Reto Brun, Manoj Munde, W. David Wilson, Sandra Nzimiro, Serene Samyesudhas, Karl A. Werbovetz, David W. Boykin,