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[Synthesis, chemical and toxicological study of a new benzimidazol derivative].
- Source :
-
Annales pharmaceutiques francaises [Ann Pharm Fr] 2009 Mar; Vol. 67 (2), pp. 78-83. Date of Electronic Publication: 2009 Jan 20. - Publication Year :
- 2009
-
Abstract
- Hydatidosis is a cosmopolitan parasitic disease that remains a real public health problem in highly endemic countries. Surgery is the mainstay treatment, but with significant morbidity and mortality. In addition, contraindications for surgery emphasize the importance of developing effective medications. Currently, albendazole is the main anti-hydatid agent used worldwide. It has proven efficacy but limited bioavailability due to weak absorption. In order to improve the bioavailability of this molecule we synthesized an ester of albendazole, which exhibits a totally modified solubility compared with the princeps compound. This synthesis was achieved with an output of 75%. The structure of the synthetic product was established by IR spectrometry and by proton nuclear magnetic resonance. A careful toxicity study revealed that this product has little toxicity when administered intraperitoneally and orally in mice, with a lethal dose 50 of 2,500 mg/kg per os and 2,250 mg/kg intraperitoneally, values comparable to those of albendazole. This in vitro parasitological study demonstrated that the chemical changes introduced on the albendazole molecule had no effect on its antiparasitic activity.
- Subjects :
- Animals
Antiparasitic Agents therapeutic use
Benzimidazoles therapeutic use
Body Weight drug effects
Echinococcosis parasitology
Indicators and Reagents
Lethal Dose 50
Mice
Antiparasitic Agents chemical synthesis
Antiparasitic Agents toxicity
Benzimidazoles chemical synthesis
Benzimidazoles toxicity
Echinococcosis drug therapy
Subjects
Details
- Language :
- French
- ISSN :
- 0003-4509
- Volume :
- 67
- Issue :
- 2
- Database :
- MEDLINE
- Journal :
- Annales pharmaceutiques francaises
- Publication Type :
- Academic Journal
- Accession number :
- 19298890
- Full Text :
- https://doi.org/10.1016/j.pharma.2008.11.001