- Synthesis, characterization and antileishmanial studies of some bioactive heteroleptic pentavalent antimonials
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In pursuit of safe drug candidates for the treatment of parasitic diseases like leishmaniasis, a series of heteroleptic pentavalent antimonials of the type [R3Sb(O2CR′)2] (1–9) have been synthesized and characterized using elemental analysis (CHN), Fourier transform infrared spectroscopy and multinuclear (1H and 13C) NMR spectroscopy. The carboxylates studied are predominantly substituted benzoates with some complexes having acetato or nicotinato ligands. The crystal structures of [Sb(C6H5)3(o-NH2C6H4COO)2] (1) and [Sb(C6H5)3(3,5-Cl2C6H3COO)2] (4) were determined as essentially monomeric with an Sb(V) centre and shown to adopt geometries intermediate between trigonal bipyramidal and square pyramidal. The antileishmanial activity was assessed against Leishmania tropica KWH23, and also human macrophages were used to measure the cytotoxicity of these complexes. The IC50 of the antimonials 1–9 indicates their efficaciousness as compared with the standard antimonial drug used. The significant activity of complex 1 assumes that greater multitude of interactions is the cause of enhanced antileishmanial activity. Cytotoxicity results showed that these antimonials are highly active even at low concentrations and are biocompatible with human macrophages, making them promising drug candidates for further investigations in this field.
- Mushtaq, Rabia,Rauf, Muhammad Khawar,Bolte, Michael,Nadhman, Akhtar,Badshah, Amin,Tahir, Muhammad Nawaz,Yasinzai, Masoom,Khan, Khalid Mohammed
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- Synthesis and structure of triphenylantimony dipropionate
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Triphenylantimony dipropionate Ph3Sb[OC(O)C2H5]2 was prepared by reacting triphenylantimony dibromide with sodium salt of propionic acid in toluene at 90°C. The structure of the compound was determined by X-ray diffraction. The coordination of the Sb atom in the compound is a trigonal bipyramid with the carboxylic groups in the axial positions. The Sb(1)-C(Ph)eq distances vary in the 2.099(7)-2.135(6) A range; the Sb(1)-O(1,3) distances are 2.113(5) and 2.109(5) A, respectively. The value of the O(1)Sb(1)O(3) axial angle is 175.0(2)°.
- Sharutin,Sharutina,Pakusina,Platonova,Fukin,Zakharov
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- Pd-catalyzed C-arylation of unsaturated compounds with pentavalent triarylantimony dicarboxylates
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Triarylantimony (V) derivatives Ar3SbX2 (X = Hal or acyloxy) were prepared by reaction of Ar3Sb with equimolar amounts of a peroxide ROOH (R = t-Bu, H) in the presence of an acid or an anhydride in good to excellent yields. Ar3Sb(O2CR)2 are mild and efficient C-arylation reagents of unsaturated compounds (methyl acrylate, styrene, 2-phenylpropene and acrylonitrile) under palladium catalysis at 50 °C, with PdCl2 being the most effective catalyst. Ar3SbHal2 do not react under these conditions.
- Moiseev, Dmitry V.,Gushchin, Aleksey V.,Shavirin, Andrey S.,Kursky, Yury A.,Dodonov, Viktor A.
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p. 176 - 184
(2007/10/03)
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