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Issue 48, 2013
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Anti-leishmanial activity of heteroleptic organometallic Sb(V) compounds

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In seeking new drugs for the treatment of the parasitic disease Leishmaniasis, an extensive range of organometallic antimony(V) dicarboxylates of the form [SbR3(O2CR′)2] have been synthesised, characterised and evaluated. The organometallic moieties (R) in the complexes vary in being Ph, tolyl (o, m or p), or benzyl. The carboxylates are predominantly substituted benzoates with some compounds incorporating acetato or cinnamato ligands. The crystal structures of [Sb(p-Tol)3(O2CC6H2-3,4,5-(OMe)3)2]·0.5PhMe and [SbPh3(m-CH3C6H4CH2CO2)2] were determined and shown to adopt a typical trigonal pyramidal geometry, being monomeric with a five coordinate Sb centre. In total, the biological activity of 26 Sb(V) compounds was assessed against the Leishmania major parasite, and also human fibroblast skin cells to give a measure of general toxicity. Of these, 11 compounds (predominantly substituted benzoates with m- or p-tolyl ligands) proved to be highly effective against the parasite amastigotes at concentrations of 0.5–3.5 μM, while being non-toxic towards the mammalian cells at levels below 25 μM, making them highly promising drug candidates.

Graphical abstract: Anti-leishmanial activity of heteroleptic organometallic Sb(v) compounds

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Publication details

The article was received on 28 May 2013, accepted on 11 Sep 2013 and first published on 27 Sep 2013

Article type: Paper
DOI: 10.1039/C3DT51382C
Citation: Dalton Trans., 2013,42, 16733-16741
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    Anti-leishmanial activity of heteroleptic organometallic Sb(V) compounds

    M. I. Ali, M. K. Rauf, A. Badshah, I. Kumar, C. M. Forsyth, P. C. Junk, L. Kedzierski and P. C. Andrews, Dalton Trans., 2013, 42, 16733
    DOI: 10.1039/C3DT51382C

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