Evaluation of the antiparasitic activities of imidazol-2-ylidene-gold(I) complexes

Archiv der Pharmazie
Waleed S KokoBernhard Biersack

Abstract

A series of cationic gold(I)-carbene complexes with various 4,5-diarylimidazolylidene ligands were either newly prepared or repurposed for testing against protozoal Leishmania major, Toxoplasma gondii, and Trypanosoma brucei parasites. The syntheses of the new complexes 1b and 1c were described. Ferrocene compound 1a showed the highest activities against L. major amastigotes and T. gondii and distinct selectivity for T. gondii cells when compared with the activity against nonmalignant Vero cells. The ferrocene derivatives 1a-c are generally more active against the L. major amastigotes and the T. gondii tachyzoites than the other tested anisyl gold complexes and the approved drugs atovaquone and amphotericin B. Compounds 1a and 1e showed the highest selectivities for L. major amastigotes. Compounds 1d and 1f showed the highest selectivities for L. major promastigotes; 1f was the most active compound against L. major promastigotes of this series of compounds. The 3,4,5-trimethoxyphenyl analog 1b also exhibited a much greater selectivity for T. b. brucei cells when compared with its activity against human HeLa cells.

References

Dec 26, 2001·Chemical Reviews·C F Shaw III
Apr 29, 2008·Journal of Ethnopharmacology·W S KokoM Iqbal Choudhary
Jul 16, 2008·International Journal of Antimicrobial Agents·Kyung-Min ChoiJisoo Yun
Nov 21, 2008·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Faustine DubarChristophe Biot
Mar 19, 2014·Bioorganic & Medicinal Chemistry Letters·Angela Maria Arenas VelásquezRegina Maria Barretto Cicarelli
Jan 29, 2016·Dalton Transactions : an International Journal of Inorganic Chemistry·Claire S Allardyce, Paul J Dyson
Oct 21, 2016·Chemistry : a European Journal·Julienne K MuenznerRainer Schobert
Jan 4, 2017·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Peter Mubanga CheukaKelly Chibale
May 20, 2017·Molecular and Biochemical Parasitology·Isabel WinterBernhard Biersack
Aug 5, 2017·Tropical Medicine and Infectious Disease·Amal K Mitra, Anthony R Mawson
Nov 27, 2018·Chemical Society Reviews·Malka MoraRenso Visbal
Sep 20, 2019·Archiv der Pharmazie·Ibrahim Al NasrBernhard Biersack

❮ Previous
Next ❯

Related Concepts

Related Feeds

African Trypanosomiasis

African trypanosomiasis, also known as sleeping sickness, is an insect-borne parasitic disease of humans and other animals. It is caused by protozoa of the species Trypanosoma brucei and almost invariably progresses to death unless treated. Discover the latest research on African trypanosomiasis here.

© 2021 Meta ULC. All rights reserved