N,N-dibenzyl-N'-benzylidenehydrazines: potent competitive glucose-6-phosphatase catalytic enzyme inhibitors.
A novel class of N,N-dibenzyl-N'-benzylidenehydrazines as potent and competitive glucose-6-phosphatase catalytic site inhibitors are described. Optimisation of this series identified compounds with IC(50) values as low as 170 nM.
Madsen
P
P
Medicinal Chemistry Research, Novo Nordisk A/S, Novo Nordisk Discovery, Novo Nordisk Park, DK-2760, Maaloev, Denmark. pem@novonordisk.com
Jakobsen
P
P
Westergaard
N
N
D001667:Binding, Competitive; D020134:Catalytic Domain; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D005952:Glucose-6-Phosphatase / Q000037:antagonists & inhibitors* / Q000378:metabolism; D006834:Hydrazines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D004791:Enzyme Inhibitors; D006834:Hydrazines; C010373:benzylidinohydrazine; D005952:Glucose-6-Phosphatase