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

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.

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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.

Item ID: 31745
Item Type: Article (Refereed Research - C1)
ISSN: 1477-9234
Funders: Australian Research Council (ARC), Quaid-i-Azam University, Higher Education Commission of Pakistan, Monash University, Higher Education Commission of Pakistan
Projects and Grants: ARC (DP110103812), QiAU Research Project no. 20-1826/NRPU/R&D
Date Deposited: 26 Feb 2014 09:39
FoR Codes: 03 CHEMICAL SCIENCES > 0302 Inorganic Chemistry > 030204 Main Group Metal Chemistry @ 100%
SEO Codes: 97 EXPANDING KNOWLEDGE > 970103 Expanding Knowledge in the Chemical Sciences @ 100%
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