28978-09-8Relevant articles and documents
Gold(I) Phosphine Derivatives with Improved Selectivity as Topically Active Drug Leads to Overcome 5-Nitroheterocyclic Drug Resistance in Trichomonas vaginalis
Miyamoto, Yukiko,Aggarwal, Shubhangi,Celaje, Jeff Joseph A.,Ihara, Sozaburo,Ang, Jonathan,Eremin, Dmitry B.,Land, Kirkwood M.,Wrischnik, Lisa A.,Zhang, Liangfang,Fokin, Valery V.,Eckmann, Lars
, p. 6608 - 6620 (2021/05/29)
Trichomonas vaginalis causes the most common, nonviral sexually transmitted infection. Only metronidazole (Mz) and tinidazole are approved for treating trichomoniasis, yet resistance is a clinical problem. The gold(I) complex, auranofin, is active against T. vaginalis and other protozoa but has significant human toxicity. In a systematic structure-activity exploration, we show here that diversification of gold(I) complexes, particularly as halides with simple C1-C3 trialkyl phosphines or as bistrialkyl phosphine complexes, can markedly improve potency against T. vaginalis and selectivity over human cells compared to that of the existing antirheumatic gold(I) drugs. All gold(I) complexes inhibited the two most abundant isoforms of the presumed target enzyme, thioredoxin reductase, but a subset of compounds were markedly more active against live T. vaginalis than the enzyme, suggesting that alternative targets exist. Furthermore, all tested gold(I) complexes acted independently of Mz and were able to overcome Mz resistance, making them candidates for the treatment of Mz-refractory trichomoniasis.
Late transition metal oxo and imido complexes. II. Gold(I) oxo complexes
Yang, Yi,Ramamoorthy, Visalakshi,Sharp, Paul R.
, p. 1946 - 1950 (2008/10/08)
The gold(I) oxo complexes [(LAu)3(μ3-O)] BF4 (1) have been prepared for L = PMePh2, PMe2Ph, PEtPh2, PPriPh2, P(p-ClPh)3, P(o-tol)3, P(OEt)Ph2, and P(OMe)3. Two of these new oxo complexes, as well as a new crystal form of [(PPh3Au)3(μ3-O)]BF4, were structurally characterized. Crystals of [(PMePh2Au)3(μ3-O)]BF 4·CH2Cl2 from CH2Cl2/ether are monoclinic (P21/c) with a= 11.395(2) A?, b = 25.901(2) A?, c = 16.024(3) A?, β = 110.615(8)°, and Z = 4. Crystals of [(PPh3Au)3(μ3-O)]BF 4·1.5CH2Cl2 from CH2Cl2/ether are monoclinic (P21/c) with a = 14.723(3) A?, b = 14.808(3) A?, c = 25.999(3) A?, β = 104.06(3)°, and Z = 4. Crystals of [(P(O-tol)3Au)3(μ3-O)]BF 4·xC6H14·0.5H2O from CH2Cl2/hexane are monoclinic (P21/a) with a = 14.2611(45) A?, b = 27.4668(71) A?, c = 23.0907(81) A?, β = 91.37(2)°, and Z = 4. The PPh3 and the PMePh2 structures consist of inversion-related edge-bridged [(LAu)3O]+ dimers held together by Au-Au interactions. The P(o-tol)3 structure consists of isolated [(LAu)3O]+ units. New oxo complexes are also formed in equilibrium mixtures of [((PPh3)Au)3(μ3-O)]BF4 and LAuCl. Oxygen-17 NMR data for 1 show chemical shifts of +19.7 to -36.0 ppm (H2O reference) with upfield shifts corresponding to increasing basicity of the phosphine, L.
Syntheses and Structure of Re(NAuCl)Cl2(PMe2Ph)3, a Complex with a Nitrido Bridge between Rhenium(V) and Gold(I)
Beuter, Georg,Englert, Ullrich,Straehle, Joachim
, p. 145 - 148 (2007/10/02)
Re(NAuCl)Cl2(PMe2Ph)3 (1) is formed by the reaction of Re(N)Cl2(PMe2Ph)3 with Au(CO)Cl in toluene at 5 deg C. 1 is an air-stable, red compound that decomposes on heating to ReNCl2(PMe2Ph)2 and Me2PhPAuCl.Recrystallization from toluene yields the solvate 1*0.5C6H5CH3.It crystallizes in the monoclinic space group P21/c with the lattice constants a = 1301.5(4), b = 939.2(4), c = 2735.0(8) pm, β = 102.79(3) deg and Z = 4.The structure is built by monomeric complexes of 1 and non-coordinated toluene molecules.The Re atom is within a pseudo-octahedral coordination with the phosphine ligands in meridional arrangement and the N-Au-Cl group trans to one Cl ligand.The Re=N-Au-Cl moiety is almost linear with bond angles of ReN-Au = 173.8 deg, N-Au-Cl = 178.9 deg and a ReN triple bond of 167.4 pm. - Keywords: Tris(dimethylphenylphosphine)dichlororhenium(V)-μ-nitrido-gold(I)chloride, Synthesis, Crystal Structure, IR Spectra
