Synthesis and antiparasitic activity of albendazole and mebendazole analogues.

نویسندگان

  • Gabriel Navarrete-Vázquez
  • Lilián Yépez
  • Alicia Hernández-Campos
  • Amparo Tapia
  • Francisco Hernández-Luis
  • Roberto Cedillo
  • José González
  • Antonio Martínez-Fernández
  • Mercedes Martínez-Grueiro
  • Rafael Castillo
چکیده

Albendazole (Abz) and Mebendazole (Mbz) analogues have been synthesized and in vitro tested against the protozoa Giardia lamblia, Trichomonas vaginalis and the helminths Trichinella spiralis and Caenorhabditis elegans. Results indicate that compounds 4a, 4b (Abz analogues), 12b and 20 (Mbz analogues) are as active as antiprotozoal agents as Metronidazole against G. lamblia. Compound 9 was 58 times more active than Abz against T. vaginalis. Compounds 8 and 4a also shown high activity against this protozoan. Compounds 4b and 5a were as active as Abz. None of the Mbz analogues showed activity against T. vaginalis. The anthelmintic activity presented by these compounds was poor.

برای دانلود متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید

ثبت نام

اگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید

منابع مشابه

Echinococcus multilocularis alkaline phosphatase as a marker for metacestode damage induced by in vitro drug treatment with albendazole sulfoxide and albendazole sulfone.

Alveolar echinococcosis (AE) is caused by the metacestode stage of the fox tapeworm Echinococcus multilocularis. The disease affects the human liver and occasionally other organs and is fatal if treatment is unsuccessful. The present chemotherapy of AE is based on the administration of benzimidazole carbamate derivatives, such as mebendazole and albendazole. Albendazole treatment has been found...

متن کامل

In vivo effect of albendazole and mebendazole on hydatid cyst of mice

In current study, a few sheep cystic livers and lungs were obtained from Mashhad slaughter house and protoscolex were separated aseptically. Thirty 6-week-old Swiss mice were divided into 5 groups and two thousands of live protoscolices were inoculated intrapritoaneally in each mouse. In group 1 and 2 (prophylactic groups), mice were given 150 mg/kg of oral albendazole and mebendazole for 10 da...

متن کامل

Deworming Campaign in Eastern Afghanistan – Prevalence of Intestinal Parasites and Adoption of Treatment Strategy

Purpose: To estimate the prevalence and species of intestinal parasites in an Afghan community as well as to establish appropriate treatment method for each of the detected pathogens. Methods: Parasitological examination of stool samples collected from 777 children aged 1-17 years, treated in Ghazni Provincial Hospital (eastern Afghanistan) conducted in the period 2012 2013 made it possible to ...

متن کامل

HPLC method for identification and quantification of benzimidazole derivatives in antiparasitic drugs.

The subject of the study was to develop a versatile HPLC system for identification and determination of four benzimidazole derivatives in the antiparasitic drugs. The tests covered: Zentel, Panacur, Vermox tablets and Systamex suspension. A satisfactory separation was obtained using the Nucleosil C8 column in the gradient system composed of mobile phase A: 85% orthophosphoric acid / water / ace...

متن کامل

Activity of benzimidazoles against Dientamoeba fragilis (Trichomonadida, Monocercomonadidae) in vitro and correlation of beta-tubulin sequences as an indicator of resistance

Recently, Dientamoeba fragilis has emerged as a significant and common enteropathogen. The majority of patients with dientamoebiasis present with gastrointestinal complaints and chronic symptoms are common. Numerous studies have successfully demonstrated parasite clearance, coupled with complete resolution of clinical symptoms following treatment with various antiparasitic compounds. Despite th...

متن کامل

ذخیره در منابع من


  با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید

برای دانلود متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید

ثبت نام

اگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید

عنوان ژورنال:
  • Bioorganic & medicinal chemistry

دوره 11 21  شماره 

صفحات  -

تاریخ انتشار 2003