Drug resistance in Giardia duodenalis

Ansell, Brendan R E; McConville, Malcolm J.; Ma’ayeh, Showgy Y.; Dagley, Michael J; Gasser, Robin B.; Svärd, Staffan G.; Jex, Aaron R.

doi:10.1016/j.biotechadv.2015.04.009

Cited by 97 publications

(112 citation statements)

References 166 publications

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“…Unfortunately, no protective vaccines are available for human use and drug therapy options have varying efficacies [6, 7]. Although Giardia infections typically resolve within a few weeks, infections may also last for several months as chronic infections.…”

Section: The Impact Of Giardiasismentioning

confidence: 99%

The Intersection of Immune Responses, Microbiota, and Pathogenesis in Giardiasis

Fink

Singer

2017

Trends in Parasitology

105

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Giardia lamblia is one of the most common infectious protozoans in the world. Giardia rarely causes severe life-threatening diarrhea, and may even have a slight protective effect in this regard, but it is a major contributor to malnutrition and growth faltering in children in the developing world. Giardia infection also appears to be a significant risk factor for post-infectious irritable bowel and chronic fatigue syndromes. In this review we highlight recent work focused on the impact of giardiasis and the mechanisms that contribute to the various outcomes of this infection, including changes in the composition of the microbiota, activation of immune responses, and immunopathology.

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Section: The Impact Of Giardiasismentioning

confidence: 99%

The Intersection of Immune Responses, Microbiota, and Pathogenesis in Giardiasis

Fink

Singer

2017

Trends in Parasitology

105

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“…However, treatment failure (especially with MTZ) has been reported due to several factors including non-compliance to the therapy, immune deficiency or drug resistance. So, the development of optimized and efficacious therapies represents an unmet medical need and optimized therapies and novel antigiardial compounds are highly needed [4].…”

Section: Introductionmentioning

confidence: 99%

Structural characterization of Giardia duodenalis thioredoxin reductase ( g TrxR) and computational analysis of its interaction with NBDHEX

Brogi¹,

Fiorillo

Chemi³

et al. 2017

European Journal of Medicinal Chemistry

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“…The colonization of the human small intestine by G. lamblia causes diarrhea, epigastric pain, nausea, vomiting, cramps, and weight loss [3]. Chronic giardiasis leads to malabsorption syndrome associated malnutrition, including failure-to-thrive in children.…”

Section: Giardiasis Is An Intestinal Infection In Humans Bymentioning

confidence: 99%

Synthesis and <i>in vitro</i> antiprotozoal activity of some 2- amino-4-phenyloxazole derivatives

Carballo¹,

Patrón-Vázquez²,

Cáceres-Castillo³

et al. 2017

Trop. J. Pharm Res

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Purpose: To prepare some 2-amino-4-(p-substituted phenyl)-oxazole derivatives and to evaluate their in vitro antiprotozoal activity against Giardia lamblia and Trichomonas vaginalis. Methods: The 2-amino-4-(p-substituted phenyl)-oxazoles (a-g) were synthesized by microwave (MW) irradiation of mixtures of p-substituted 2-bromoacetophenones and urea in dimethylformamide (DMF). All compounds were identified by 1 H and 13 C nuclear magnetic resonance (NMR) spectroscopy and lowand high-resolution mass spectrometry (HRMS). NMR assignments were made based on heteronuclear single quantum coherence (HSQC) and heteronuclear multiple bond correlation (HMBC) experiments. Each synthesized compound's melting point was determined. Antiprotozoal activity against Giardia intestinalis and Trichomonas vaginalis was quantified using a rigorous and sensitive subculture method. The commercial drug, metronidazole, was used as positive control. The 50 % inhibitory concentration (IC50) of the antiprotozoal agents for each protozoa was determined. Results: Seven 2-amino-4-(p-substituted phenyl)-oxazoles (a-g) were synthesized. The most active compounds against G. lamblia was 2-amino-4-(p-benzoyloxyphenyl)-oxazole (3d) with an IC50 of 1.17 µM, while compound 3e (2-amino-4-(p-bromophenyl)-oxazole) showed the highest anti-trichomonal activity (IC50, 1.89 µM). Conclusion: The in vitro antigiardial activity of 2-amino-4-(p-benzoyloxyphenyl) oxazole was higher than that exhibited by metronidazole; however, it is necessary increase the number of synthetic derivatives in order to be able to determine their structure-activity relationship.

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Drug resistance in Giardia duodenalis

Cited by 97 publications

References 166 publications

The Intersection of Immune Responses, Microbiota, and Pathogenesis in Giardiasis

The Intersection of Immune Responses, Microbiota, and Pathogenesis in Giardiasis

Structural characterization of Giardia duodenalis thioredoxin reductase ( g TrxR) and computational analysis of its interaction with NBDHEX

Synthesis and <i>in vitro</i> antiprotozoal activity of some 2- amino-4-phenyloxazole derivatives

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