Author/Authors :
Laixing Hu، نويسنده , , Reem K. Arafa، نويسنده , , Mohamed A. Ismail، نويسنده , , Tanja Wenzler، نويسنده , , Reto Brun، نويسنده , , Manoj Munde، نويسنده , , W. David Wilson، نويسنده , , Sandra Nzimiro، نويسنده , , Serene Samyesudhas، نويسنده , , Karl A. Werbovetz، نويسنده , , David W. Boykin، نويسنده ,
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.
Keywords :
Leishmania , Diamidines , Azaterphenyl , DNA binding , Suzuki coupling
