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

作者：Louie Theola; Goodman C Dean; Holloway Georgina A; McFadden Geoffrey I; Mollard Vanessa; Watson Keith G^*

来源：Bioorganic & Medicinal Chemistry Letters, 2010, 20(15): 4611-4613.

DOI：10.1016/j.bmcl.2010.06.007

• Acetyl-CoA carboxylase
• Antimalarial
• 1,3-Cyclohexanedione

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 mu M. 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 mu M.

• 出版日期2010-8-1
• 单位河北医科大学