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Merck
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
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.

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Sigma-Aldrich
1,3-环己二酮, 97%
Supelco
喹禾灵, PESTANAL®, analytical standard