Abstract
The application of BN/CC isosterism is explored as a method of expanding the scope of core scaffolds in biologically active compounds. The viability of potential drug candidates incorporating BN-heteroaromatic moieties was investigated through the synthesis of BN-substituted analogs to known phosphodiesterase (PDE10A) inhibitors, namely MP10 and a selection of N-methylanilide analogs. These in some cases revealed unexpectedly potent and relatively stable derivatives, providing further support for the potential of BN-incorporation in medicinal chemistry.
Keywords:
Antipsychotics; Borazaronaphthalenes; PDE10A inhibitors.
Copyright © 2015 Elsevier Ltd. All rights reserved.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Antipsychotic Agents / chemical synthesis
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Antipsychotic Agents / chemistry*
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Antipsychotic Agents / metabolism
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Binding Sites
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Catalytic Domain
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Humans
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Molecular Docking Simulation
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Naphthalenes / chemical synthesis
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Naphthalenes / chemistry*
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Naphthalenes / metabolism
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Phosphodiesterase Inhibitors / chemical synthesis
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Phosphodiesterase Inhibitors / chemistry*
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Phosphodiesterase Inhibitors / metabolism
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Phosphoric Diester Hydrolases / chemistry*
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Phosphoric Diester Hydrolases / metabolism
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Protein Binding
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Structure-Activity Relationship
Substances
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Antipsychotic Agents
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Naphthalenes
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Phosphodiesterase Inhibitors
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PDE10A protein, human
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Phosphoric Diester Hydrolases