Regresar

Thiophenes as mosquito larvicides: Structure-toxicity relationship analysis

Abstract:

The phototoxicity and non-light-mediated toxicity of 41 naturally occurring and synthetic tricyclic thiophenes was assessed against larvae of the mosquito Aedes atropalpus. Seventeen of the tested compounds were extremely potent, with LC50 values for phototoxicity in the nanomolar range. The role of the thiophenes' physicochemical properties, such as hydrophobicity and ability to produce singlet oxygen, with regard to their larvicidal activity was investigated using quantitative structure-activity analysis. It was found that 84% of the variation in phototoxicity could be explained by a combination of the logarithm of octanol/water partition coefficients and the rate of singlet oxygen production. Comparison of this model with one derived for phototoxicity to nauplii of the brine shrimp (Artemia salina) suggests the possibility of achieving some degree of species selectivity by manipulation of the lipophilic character of the tricyclic thiophenes. © 1991.

Año de publicación:

1991

Keywords:

    Fuente:

    scopusscopus

    Tipo de documento:

    Article

    Estado:

    Acceso restringido

    Áreas de conocimiento:

    • Descubrimiento de fármacos
    • Biología

    Áreas temáticas:

    • Microorganismos, hongos y algas
    • Farmacología y terapéutica
    • Fisiología humana

    Contribuidores:

    Duval F.Duval F.
    Marles R.J.Marles R.J.
    Scaiano J.C.Scaiano J.C.
    Cesar M. CompadreCesar M. Compadre
    Morand P.Morand P.
    Mehta B.Mehta B.
    Soucy‐Breau C.Soucy‐Breau C.
    Arnason J.T.Arnason J.T.
    Redmond R.W.Redmond R.W.
    Compadre R.L.Compadre R.L.