Synthesis and antiprotozoal activity of novel 1-methylbenzimidazole derivatives.

doi:10.1016/j.bmc.2008.12.059

Paper

Synthesis and antiprotozoal activity of novel 1-methylbenzimidazole derivatives.

Published Feb 15, 2009 · David Valdez-Padilla, S. Rodríguez-Morales, A. Hernández-Campos

Bioorganic & medicinal chemistry

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63

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Abstract

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In Vitro Study

Study Snapshot

Novel 1-methylbenzimidazole derivatives show greater antiprotozoal activity than metronidazole against Giardia intestinalis and Trichomonas vaginalis, with the most active group being those with a 2-ethoxycarbonyl group.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Paper

Synthesis and antiprotozoal activity of novel 1-methylbenzimidazole derivatives.

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References

Alternate Method for the Synthesis of N‐Alkyl/aralkyl‐2‐(α‐hydroxy Alkyl/aralkyl)benzimidazoles via Regiospecific Acetylation

Acetylation of 1H-(hydroxyalkyl/aryl)benzimidazoles with Ac2O leads to the regiospecific formation of O-acetoxy derivative 3, which can be alkylated to N-alkyl derivatives 4 for the synthesis of the title compounds.

Treatment options for the eradication of intestinal protozoa

Intestinal protozoa can cause severe diarrhea and can be effectively treated with various medications, including co-trimoxazole, microsporidia, and nitazoxanide.

Synthesis and antiprotozoal activity of some 2-(trifluoromethyl)-1H-benzimidazole bioisosteres.

Compound 4 is 14 times more active than albendazole against Trichomonas vaginalis, showing potential antimalarial activity against Plasmodium falciparum.

Use of Trichomonas vaginalis Clinical Isolates to Evaluate Correlation of Gene Expression and Metronidazole Resistance

No significant correlation was found between gene expression and metronidazole resistance or susceptibility in Trichomonas vaginalis clinical isolates.

5-Nitroimidazole Drugs Effective against Metronidazole-Resistant Trichomonas vaginalis and Giardia duodenalis

5-nitroimidazole drugs show potential in inhibiting metronidazole-resistant Giardia and Trichomonas, potentially overcoming cross-resistance among existing antiparasitic drugs.

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