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Effect of the lipophilic parameter (log P) on the anti-parasitic activity of imidazo[1,2-a]pyridine derivatives

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Abstract

A number of imidazo[1,2-a]pyridine derivatives were selected and investigated in relation to anti-parasitic (Trichomonas vaginalis) activity. After treatment with derivatives, biological activity was assessed by determination of the in vitro viability of cell cultures, using alamar blue as a metabolic indicator. A good correlation was found between the anti-parasitic activity and the partition coefficient log P determined experimentally on the tested compounds, which explained up to 84% of the measured activity. A favorable interval (0.9 ± 0.3 log P) was found for optimum biological response.

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Acknowledgments

Financial support through grant No. 49937, Consejo Nacional de Ciencia y Tecnología (CONACYT) México is gratefully acknowledgedSpecial thanks to Dr. Marco Meráz, Departamento Biología Molecular, CINVESTAV México for kindly providing the strains of Trichomonas vaginalis

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Authors and Affiliations

  1. Departamento Química Orgánica, Escuela Nacional Ciencias Biológicas, IPN, Prolongación Carpio y Plan de Ayala S/N, 11340, Mexico, DF, Mexico

    Margarita López-Martínez, Héctor Salgado-Zamora, Ma. Elena Campos-Aldrete & Carlos Mexica-Ochoa

  2. Laboratorio de Modelado Molecular y Bioinformática, SEPI, Escuela Superior de Medicina, IPN, Plan de San Luis y Díaz Mirón, 11340, Mexico, DF, Mexico

    José G. Trujillo-Ferrara & José Correa-Basurto

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  1. Margarita López-Martínez
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  2. Héctor Salgado-Zamora
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  3. Ma. Elena Campos-Aldrete
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  4. José G. Trujillo-Ferrara
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  5. José Correa-Basurto
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  6. Carlos Mexica-Ochoa
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Correspondence to Héctor Salgado-Zamora.

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López-Martínez, M., Salgado-Zamora, H., Campos-Aldrete, M.E. et al. Effect of the lipophilic parameter (log P) on the anti-parasitic activity of imidazo[1,2-a]pyridine derivatives. Med Chem Res 21, 415–420 (2012). https://doi.org/10.1007/s00044-010-9547-3

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  • DOI: https://doi.org/10.1007/s00044-010-9547-3

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