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Acta Pharmaceutica Sinica ; (12): 700-704, 2002.
Article in Chinese | WPRIM | ID: wpr-312033

ABSTRACT

<p><b>AIM</b>To synthesize novel derivatives of hydroxylbenzenedisulfonanilide with high insecticidal activity against the Fasciola hepatica.</p><p><b>METHODS</b>o-(m-, p-) Chlorphenol were used to synthesize the title compounds by sulphonation and nucleiphilic-substitution reaction. The uncoupling activity (insecticidal activity) of these compounds were tested by determining the influence on mitochondrial respiration control ratio (RCR) and the variation of inorganic phosphate in oxidative phosphorylation (delta Pi).</p><p><b>RESULTS</b>Compounds 1-14 are new compounds. The structures of the compounds were determined by IR, HNMR and elemental analysis. Most new compounds have relatively high uncoupling activities, especially compounds 3, 5, 6 and 9.</p><p><b>CONCLUSION</b>Compounds 3, 5, 6 and 9 will become novel fasciolicides and are worth further studying.</p>


Subject(s)
Animals , Anilides , Chemistry , Pharmacology , Anthelmintics , Chemistry , Pharmacology , Fasciola hepatica , Mitochondria, Liver , Physiology , Molecular Structure , Oxygen Consumption , Sulfonamides , Chemistry , Pharmacology
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