Synthesis and fungicidal activity of novel 2-oxocycloalkylsulfonylureas

J Agric Food Chem. 2005 Mar 23;53(6):2202-6. doi: 10.1021/jf0403944.

Abstract

A series of 2-oxocycloalkylsulfonylureas (2) have been synthesized in a six-step, three-pot reaction sequence from readily available cyclododecanone, cycloheptanone, and cyclohexanone. Their structures were confirmed by IR, 1H NMR, and elemental analysis. The bioassay indicated that some of them possess certain fungicidal activity against Gibberella zeae Petch. In general, compounds containing a 12-membered ring (2A) are more active than those containing a 6- or 7-membered ring (2B, 2C). In the series 2A, the compounds in which R is a disubstituted phenyl or pyrimidyl showed better activity than those in which R is a monosubstituted phenyl or pyrimidyl, and aryl-substituted compounds have somewhat higher activity than those substituted by pyrimidyl. The further bioassay showed that the representative of 2A, 2A15, has good fungicidal activities against not only G. zeae Petch but also Botrytis cinerea Pers, Colletotrichum orbiculare Arx, Pythium aphanidermatum Fitzp, Fusarium oxysporum Schl. f. sp. Vasinfectum, etc.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Fungi / drug effects
  • Fungicides, Industrial / chemical synthesis*
  • Fungicides, Industrial / pharmacology*
  • Gibberella / drug effects
  • Magnetic Resonance Spectroscopy
  • Molecular Structure
  • Quantitative Structure-Activity Relationship
  • Sulfonylurea Compounds / chemical synthesis*
  • Sulfonylurea Compounds / pharmacology*

Substances

  • Fungicides, Industrial
  • Sulfonylurea Compounds