ODependent efficacy of novel piperidine- And piperazine-based chalcones against the human parasite giardia intestinalis

Vijay Bahadur, Daniela Mastronicola, Hemandra K. Tiwari, Yogesh Kumar, Micol Falabella, Leopoldo P. Pucillo, Paolo Sarti, Alessandro Giuffrè, Brajendra K. Singh

Research output: Contribution to journalArticle

Abstract

Giardia intestinalis is the most frequent protozoan agent of intestinal diseases worldwide. Though commonly regarded as an anaerobic pathogen, it preferentially colonizes the fairly oxygen-rich mucosa of the proximal small intestine. Therefore, when testing new potential antigiardial drugs, Oshould be taken into account, since it also reduces the efficacy of metronidazole, the gold standard drug against giardiasis. In this study, 46 novel chalcones were synthesized by microwave-assisted Claisen-Schmidt condensation, purified, characterized by high-resolution mass spectrometry, 1H and 13C nuclear magnetic resonance, and infrared spectroscopy, and tested for their toxicity against G. intestinalis under standard anaerobic conditions. As a novel approach, compounds showing antigiardial activity under anaerobiosis were also assayed under microaerobic conditions, and their selectivity against parasitic cells was assessed in a counterscreen on human epithelial colorectal adenocarcinoma cells. Among the tested compounds, three [30(a), 31(e), and 33] were more effective in the presence of Othan under anaerobic conditions and killed the parasite 2 to 4 times more efficiently than metronidazole under anaerobiosis. Two of them [30(a) and 31(e)] proved to be selective against parasitic cells, thus representing potential candidates for the design of novel antigiardial drugs. This study highlights the importance of testing new potential antigiardial agents not only under anaerobic conditions but also at low, more physiological Oconcentrations.

Original languageEnglish
Pages (from-to)543-549
Number of pages7
JournalAntimicrobial Agents and Chemotherapy
Volume58
Issue number1
DOIs
Publication statusPublished - Jan 2014

ASJC Scopus subject areas

  • Pharmacology (medical)
  • Pharmacology
  • Infectious Diseases

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    Bahadur, V., Mastronicola, D., Tiwari, H. K., Kumar, Y., Falabella, M., Pucillo, L. P., Sarti, P., Giuffrè, A., & Singh, B. K. (2014). ODependent efficacy of novel piperidine- And piperazine-based chalcones against the human parasite giardia intestinalis. Antimicrobial Agents and Chemotherapy, 58(1), 543-549. https://doi.org/10.1128/AAC.00990-13