Azaterphenyl diamidines as antileishmanial agents

Bioorg Med Chem Lett. 2008 Jan 1;18(1):247-51. doi: 10.1016/j.bmcl.2007.10.091.

Laixing Hu ¹, 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

Affiliations

Affiliation

1 Department of Chemistry and Center for Biotechnology and Drug Design, Georgia State University, Atlanta, GA 30303, USA.

PMID: 18006310 DOI: 10.1016/j.bmcl.2007.10.091

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.

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