Aminoguanidines: New leads for treatment of Giardia duodenalis infection

Autor: Rebecca J. Abraham, Sam Abraham, Andrew J. Stevens, Stephen W. Page, Adam McCluskey, Darren J. Trott, Ryan M. O'Handley
Jazyk: angličtina
Rok vydání: 2019
Předmět:
Zdroj: International Journal for Parasitology: Drugs and Drug Resistance, Vol 10, Iss , Pp 38-44 (2019)
Druh dokumentu: article
ISSN: 2211-3207
DOI: 10.1016/j.ijpddr.2019.04.003
Popis: Giardia duodenalis is an ubiquitous parasitic pathogen that causes significant morbidity and mortality worldwide. Failures in drug therapy are commonly due to poor patient compliance as a result of the need for repeated administration, off target drug effects and increasing parasite drug resistance. In this study the in vitro efficacy and selectivity of the aminoguanidine compound robenidine and 2 structural analogues against Giardia were determined. After 5 h exposure to each compound the IC50 was as low as 0.2 μM with corresponding MLCs as low as 2.8 μM. This is in contrast to metronidazole which required 24 h to exhibit inhibitory activity. A modified adherence assay, developed for this study, demonstrated that three of the compounds inhibited in vitro adherence of the parasite. The lead compound exhibited rapid giardicidal activity (
Databáze: Directory of Open Access Journals