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[Synthesis, chemical and toxicological study of a new benzimidazol derivative].

Authors :
Ansar M
Zellou A
Faouzi ME
Zahidi A
Serroukh S
Lmimouni BE
Cherrah Y
Taoufik J
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.

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