Abstract
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.
Letters in Drug Design & Discovery
Title:Synthesis and Anthelmintic Evaluation of Novel Valerolactam- Benzimidazole Hybrids
Volume: 10 Issue: 10
Author(s): Beatriz Munguía, Pablo Mendina, Romina Espinosa, Andrea Lanz, Jenny Saldaña, María J. Andina, Ximena Ures, Andrés López, Eduardo Manta and Laura Domínguez
Affiliation:
Keywords: Anthelmintic activity, N. brasiliensis, Benzimidazole carbamates, Hybrids, Valerolactam-benzimidazoles.
Abstract: 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.
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Cite this article as:
Munguía Beatriz, Mendina Pablo, Espinosa Romina, Lanz Andrea, Saldaña Jenny, J. Andina María, Ures Ximena, López Andrés, Manta Eduardo and Domínguez Laura, Synthesis and Anthelmintic Evaluation of Novel Valerolactam- Benzimidazole Hybrids, Letters in Drug Design & Discovery 2013; 10 (10) . https://dx.doi.org/10.2174/15701808113109990028
DOI https://dx.doi.org/10.2174/15701808113109990028 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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