Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
Email: lddd@benthamscience.org


Synthesis and Anthelmintic Evaluation of Novel Valerolactam- Benzimidazole Hybrids

Author(s): Beatriz Munguía, Pablo Mendina, Romina Espinosa, Andrea Lanz, Jenny Saldaña, María J. Andina, Ximena Ures, Andrés López, Eduardo Manta, Laura Domínguez.


Some novel valerolactam derivatives of 5(6)-substituted-(1H-benzimidazol-2-yl-amine) were constructed based on the union of two structural domains with anthelmintic activity. The tested hybrid compounds 7-9 exhibited greater activity using the Nippostrongylus brasiliensis physiology-based in vitro bioassay in comparison to commercial anthelmintic benzimidazoles. Moreover, the improved physicochemical properties of hybrid compounds compared with valerolactam domain allowed the penetration of parasite barriers, concurrently with an increased intraparasitary bioavailability.

Keywords: Anthelmintic activity, N. brasiliensis, Benzimidazole carbamates, Hybrids, Valerolactam-benzimidazoles.

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Article Details

Year: 2013
Page: [1007 - 1014]
Pages: 8
DOI: 10.2174/15701808113109990028
Price: $58