Bioorganic & Medicinal Chemistry Letters 2010-08-01

Dimeric cyclohexane-1,3-dione oximes inhibit wheat acetyl-CoA carboxylase and show anti-malarial activity.

Theola Louie, C Dean Goodman, Georgina A Holloway, Geoffrey I McFadden, Vanessa Mollard, Keith G Watson

文献索引：Bioorg. Med. Chem. Lett. 20 , 4611-3, (2010)

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摘要

A series of dimeric 1,3-cyclohexanedione oxime ethers were synthesized and found to have significant antiplasmodial activity with IC(50)'s in the range 3-12 microM. The most active dimer was tested in the Plasmodium berghei mouse model of malaria and at a dose of 48 mg/kg gave a 45% reduction in parasitaemia. Several commercial herbicides, all known to be inhibitors of maize acetyl-CoA carboxylase, were also tested for antimalarial activity, but were essentially inactive with the exception of butroxydim which gave an IC(50) of 10 microM.Copyright 2010 Elsevier Ltd. All rights reserved.

相关化合物

  • 喹禾灵
  • 1,3-环己二酮

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