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

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

Bioorganic & medicinal chemistry letters (2010-06-29)
Theola Louie, C Dean Goodman, Georgina A Holloway, Geoffrey I McFadden, Vanessa Mollard, Keith G Watson
ABSTRACT

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.

MATERIALS
Product Number
Brand
Product Description

Supelco
Quizalofop-ethyl, PESTANAL®, analytical standard
Sigma-Aldrich
1,3-Cyclohexanedione, 97%