Azaterphenyl diamidines as antileishmanial agents.

Citation:
Hu, L., R. K. Arafa, M. A. Ismail, T. Wenzler, R. Brun, M. Munde, D. W. Wilson, S. Nzimiro, S. Samyesudhas, K. A. Werbovetz, et al., "Azaterphenyl diamidines as antileishmanial agents.", Bioorganic & medicinal chemistry letters, vol. 18, issue 1, pp. 247-51, 2008 Jan 1.

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.

Notes:

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