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ChemMedChem ; 9(4): 693-8, 2014 Apr.
Article in English | MEDLINE | ID: mdl-24446373

ABSTRACT

The role of the synaptic vesicle protein 2A (SV2A) protein, target of the antiepileptic drug levetiracetam, is still mostly unknown. Considering its potential to provide in vivo functional insights into the role of SV2A in epileptic patients, the development of an SV2A positron emission tomography (PET) tracer has been undertaken. Using a 3D pharmacophore model based on close analogues of levetiracetam, we report the rationale design of three heterocyclic non-acetamide lead compounds, UCB-A, UCB-H and UCB-J, the first single-digit nanomolar SV2A ligands with suitable properties for development as PET tracers.


Subject(s)
Acetamides , Drug Discovery , Heterocyclic Compounds , Membrane Glycoproteins/analysis , Nerve Tissue Proteins/analysis , Positron-Emission Tomography , Acetamides/chemical synthesis , Acetamides/chemistry , Animals , Heterocyclic Compounds/chemical synthesis , Heterocyclic Compounds/chemistry , Humans , Ligands , Male , Membrane Glycoproteins/metabolism , Models, Molecular , Molecular Structure , Nerve Tissue Proteins/metabolism , Radioactive Tracers , Rats , Rats, Wistar
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