Ali, Muhammad, Rauf, Muhammad, Badshah, Amin, Kumar, Ish, Forsyth, Craig M., Junk, Peter C., Kedzierski, Lukasz, and Andrews, Philip C. (2013) Anti-leishmanial activity of heteroleptic organometallic Sb(v) compounds. Dalton Transactions, 42 (48). pp. 16733-16741.

PDF (Published Version) - Published Version Restricted to Repository staff only

 

75

6

Abstract

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.

Actions (Repository Staff Only)

Item Control Page