N,N-dibenzyl-N'-benzylidenehydrazines: potent competitive glucose-6-phosphatase catalytic enzyme inhibitors

P Madsen; P Jakobsen; N Westergaard

doi:10.1016/s0960-894x(01)00395-x

N,N-dibenzyl-N'-benzylidenehydrazines: potent competitive glucose-6-phosphatase catalytic enzyme inhibitors

Bioorg Med Chem Lett. 2001 Aug 20;11(16):2165-7. doi: 10.1016/s0960-894x(01)00395-x.

Authors

P Madsen¹, P Jakobsen, N Westergaard

Affiliation

¹ Medicinal Chemistry Research, Novo Nordisk A/S, Novo Nordisk Discovery, Novo Nordisk Park, DK-2760, Maaloev, Denmark. [email protected]

PMID: 11514161
DOI: 10.1016/s0960-894x(01)00395-x

Abstract

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.

MeSH terms

Binding, Competitive
Catalytic Domain
Enzyme Inhibitors / chemical synthesis
Enzyme Inhibitors / chemistry
Enzyme Inhibitors / pharmacology*
Glucose-6-Phosphatase / antagonists & inhibitors*
Glucose-6-Phosphatase / metabolism
Hydrazines / chemical synthesis
Hydrazines / chemistry
Hydrazines / pharmacology*
Structure-Activity Relationship

Substances

Enzyme Inhibitors
Hydrazines
benzylidinohydrazine
Glucose-6-Phosphatase