A structural investigation of heteroleptic pentavalent antimonials and their leishmanicidal activity |
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| Authors: | Rabia Mushtaq Muhammad Khawar Rauf Marcus Bond Amin Badshah Muhammad Irshad Ali Akhtar Nadhman Masoom Yasinzai Muhammad Nawaz Tahir |
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| Affiliation: | 1. Department of Chemistry, Quaid‐i‐Azam University, Islamabad, Pakistan;2. Department of Chemistry, Southeast Missouri State University, Cape Girardeau, MO, USA;3. Department of Biotechnology, Quaid‐i‐Azam University, Islamabad, Pakistan;4. Department of Physics, University of Sargodha, Sargodha, Pakistan |
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| Abstract: | In the quest for new drug candidates for the safe treatment of parasitic diseases like leishmaniasis, a series of heteroleptic pentavalent antimonials of the type [SbR3(OOCR′)2] were synthesized and characterized using elemental analysis, Fourier transform infrared spectroscopy and multinuclear (1H and 13C) NMR spectroscopy. The carboxylate moieties are predominantly substituted benzoates with some complexes that fit in acetato or nicotinato ligands. The crystal structures of [Sb(p‐Tol)3(p‐CH3C6H4COO)2], [Sb(p‐Tol)3(3,5‐Cl2C6H3COO)2] and [Sb(p‐Tol)3(3‐nicotinato)2] were determined crystallographically and shown to adopt geometries intermediate between trigonal bipyramidal and square pyramidal, and essentially monomeric with a five‐coordinated Sb center. The leishmanicidal activity was assessed against the Leishmania tropica KWH23 parasite, and the cytotoxicity level was also measured on human macrophage blood cells. It was observed that IC50 of the antimonials was 100‐fold superior as compared with the standard antimonial drug used. Cytotoxicity results showed that these antimonials are highly active even at low concentrations and are biocompatible with human macrophages, making them highly promising drug candidates for further investigation. Copyright © 2016 John Wiley & Sons, Ltd. |
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| Keywords: | pentavalent antimonials Leishmania tropica KWH23 leishmanicidal cytotoxicity |
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