90994-24-4Relevant academic research and scientific papers
Vibrational and solid state (CP/MAS) 31P NMR spectroscopic studies of bis(trimethylphosphine)gold(I) halides
De Silva,Bowmaker,Healy
, p. 263 - 272 (2000)
The 1:2 AuX/PMe3 (X = Cl,Br,I) complexes have been prepared and studied by infrared, Raman and solid-state cross polarisation magic angle spinning (CP MAS) 31P NMR spectroscopy. The new complex bis(trimethylphosphine)iodogold(I) [AuI(PMe3)2] was prepared by the reaction of [AuI(PMe3)] with PMe3 in dimethylformamide solution. A new method for the preparation of the corresponding bromide complex [AuBr(PMe3)2], from [NBu4][AuBr2] and PMe3, is described. The IR, Raman and CP MAS 31P NMR spectra of the X = Cl, Br compounds are essentially identical, whereas those for X = I show differences that are suggestive of relatively minor differences in the crystal structure relative to the X = Cl, Br compounds. The latter compounds exist as the ionic species [Au(PMe3)2]+X-, and the X = I complex is also essentially ionic, but with a possible weak Au···I interaction; this conclusion is supported by the 197Au Mossbauer spectrum of this compound. The solid-state CP MAS 31P NMR spectra of the chloride and bromide complexes consist of doublets due to the presence of 1J(197Au-31P) coupling. This study is the first in which such coupling is observed for the P-Au-P coordination environment. The 1J(197Au-31P) coupling constants are estimated from the doublet splittings.
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.
