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Letters in Drug Design & Discovery

Author(s): Laura Scarone, Jose Fajardo, Jenny Saldana, Laura Dominguez, Pablo Esposito, Sylvia Demastteis, Peter Wipf, Eduardo Manta and Gloria Serra

DOI: 10.2174/157018009789057553

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Synthesis and Evaluation of Anthelmintic and Cytotoxic Properties of [2,5]Bis-1,3-Azole Analogs of Bengazoles

Page: [413 - 419] Pages: 7

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Abstract

Using different heterocycle formation methodologies (Deoxo-Fluor, DAST, POCl3, TosMIC), [2,5]bis-1,3- azoles were prepared as stable analogs of bengazoles, a family of potent anthelmintic marine natural products. The cytotoxic activity of these heterocycles and their precursors on HCT-15 cells and the effect on the L4 larvae of Nippostrongylus brasiliensis were evaluated.

Keywords: Bis-1, 3-azoles, Anthelmintic, Cytotoxic, Bengazoles