Synthesis and Antifungal Activity of N-Substituted-α-oxocyclododecylsulphonamides

Abstract

Abstract: Aseries of N-substituted-a-oxocyclododecylsulphonamides (Ⅲ) have been synthe-sized by amination of a-oxocyclododecylsulphonic acid chloride, obtained from the readily available cyclododecanone via a-oxocyclododecylsulphonic acid. Their structures were con-firmed by IR, MS, ¹H NMRand elementary analysis. The bioassay for antifungal activitywas carried out and all the title compounds were found to be active against Gibberella zeae.The compounds showing the highest activity are those substituted by a chlorophenyl group on the nitrogen atom (Ⅲ 8, Ⅲ 7). Their structure-activity relationship was discussed by means of conformational analysis.

Key words: N-substituted-α-oxocyclododecyl sulphonamide, Antifungal activity, Synthesis, Conformational analysis

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WANG Xiao-Ping, WANG Dao-Quan. Synthesis and Antifungal Activity of N-Substituted-α-oxocyclododecylsulphonamides[J]. Chem. J. Chinese Universities, 1997, 18(6): 889.

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Synthesis and Antifungal Activity of N-Substituted-α-oxocyclododecylsulphonamides

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