Related Products of 141556-45-8In 2022 ,《Antileishmanial activity and insights into the mechanisms of action of symmetric Au(I) benzyl and aryl-N-heterocyclic carbenes》 was published in Journal of Inorganic Biochemistry. The article was written by Rosa, Leticia B.; Galuppo, Carolina; Lima, Rochanna L. A.; Fontes, Josielle V.; Siqueira, Fabio S.; Judice, Wagner A. S.; Abbehausen, Camilla; Miguel, Danilo C.. The article contains the following contents:
Leishmania amazonensis and L. braziliensis are the main etiol. agents of the American Tegumentary Leishmaniasis (ATL). Taking into account the limited effectiveness and high toxicity of the current drug arsenal to treat ATL, novel options are urgently needed. Inspired by the fact that gold-based compounds are promising candidates for antileishmanial drugs, we studied the biol. action of a systematic series of six (1)-(6) sym. Au(I) benzyl and aryl-N-heterocyclic carbenes. All compounds were active at low micromolar concentrations with 50% effective concentrations ranging from 1.57 to 8.30 μM against Leishmania promastigotes. The mesityl derivative (3) proved to be the best candidate from this series, with a selectivity index ∼13 against both species. The results suggest an effect of the steric and electronic parameters of the N-substituent in the activity. Intracellular infections were drastically reduced after 24h of (2)-(5) incubation in terms of infection rate and amastigote burden. Further investigations showed that our compounds induced significant parasites′ morphol. alterations and membrane permeability. Also, (3) and (6) were able to reduce the residual activity of three Leishmania recombinant cysteine proteases, known as possible targets for Au(I) complexes. Our promising results open the possibility of exploring gold complexes as leishmanicidal mols. to be further screened in in vivo models of infection.1,3-Dimesityl-1H-imidazol-3-ium chloride(cas: 141556-45-8Related Products of 141556-45-8) was used in this study.
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.Related Products of 141556-45-8
Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem