Novel 5-Nitroimidazole and 5-Nitrothiazole Piperazine Derivatives and Their Antiparasitic Activity

Haythem A. Saadeh, Mohammad A. Khasawneh, Youssif A. Abu-Zeid, Ismail A. El-Haty, Mohammad S. Mubarak, Sylvain Pechangou Nsangou, Kapil Goyal, Rakesh Sehgal, José Marco-Contelles, Abdelouahid Samadi

Research output: Contribution to journalArticlepeer-review

4 Citations (Scopus)

Abstract

A novel series of 5-nitroimidazole-piperazines (4a–j) and 5-nitrothiazole-piperazine (7a–j) have been prepared in good yields. The antigiardial and antitrichomonal activities of these new compounds were evaluated. Majority of the compounds was found to be more active against Giardia lamblia as compared to metronidazole at 24 hours of incubation. After 48 hours of incubation, compounds 4b, 4f, 7c and 7j showed better activity against G. lamblia with IC50 of 15.3, 11.4, 5.9, 13.5 μM respectively compared to metronidazole (17.4 μM). Compounds 4a–j and 7a–j exhibited anti-parasitic activity against T. vaginalis with IC50 ranging from 16.4–88.7 μM and 1.2–86.7 μM at 24 hours and 48 hours of incubation respectively. Compounds 4c and 7e were 15 times more potent than the standard drug, metronidazole.

Original languageEnglish
Pages (from-to)5684-5687
Number of pages4
JournalChemistrySelect
Volume2
Issue number20
DOIs
Publication statusPublished - Jul 11 2017

Keywords

  • 5-Nitroimidazole
  • 5-Nitrothiazole
  • Antigiradia
  • Antitrichomal
  • Piperazines

ASJC Scopus subject areas

  • Chemistry(all)

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