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 published an article in 2021. The article was titled 《Gold(I) Phosphine Derivatives with Improved Selectivity as Topically Active Drug Leads to Overcome 5-Nitroheterocyclic Drug Resistance in Trichomonas vaginalis》, and you may find the article in Journal of Medicinal Chemistry.Name: 1,3-Dimesityl-1H-imidazol-3-ium chloride The information in the text is summarized as follows:
Trichomonas vaginalis causes the most common, nonviral sexually transmitted infection. Only metronidazole (Mz) and tinidazole are approved for treating trichomoniasis, yet resistance is a clin. 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, authors 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. The experimental part of the paper was very detailed, including the reaction process of 1,3-Dimesityl-1H-imidazol-3-ium chloride(cas: 141556-45-8Name: 1,3-Dimesityl-1H-imidazol-3-ium chloride)
1,3-Dimesityl-1H-imidazol-3-ium chloride(cas: 141556-45-8) is a ligand for arylation of aldehydes and for carbene catalyzed intermolecular arylation of C-H bonds. It is used as a phosphine-free ligand in various metal-catalyzed coupling reactions, often with advantageous results in difficult cases.Name: 1,3-Dimesityl-1H-imidazol-3-ium chloride
Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem