Abstract
1H-Pyrazolo[4,3-d]pyrimidines were previously disclosed as a potent second generation class of phosphodiesterase 5 (PDE5) inhibitors. This work explores the advancement of more selective and potent PDE5 inhibitors resulting from the substitution of 2-(2,2,2-trifluoroethoxy)ethyl at the 1 position in the so-called alkoxy pocket.
Copyright 2010 Elsevier Ltd. All rights reserved.
MeSH terms
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Animals
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Antihypertensive Agents / chemical synthesis
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Antihypertensive Agents / chemistry*
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Antihypertensive Agents / pharmacokinetics
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Cyclic Nucleotide Phosphodiesterases, Type 5 / metabolism
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Enzyme Inhibitors / chemical synthesis
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Enzyme Inhibitors / chemistry*
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Enzyme Inhibitors / pharmacokinetics
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Humans
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Microsomes, Liver / metabolism
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Patch-Clamp Techniques
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Phosphodiesterase 5 Inhibitors*
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Pyrimidines / chemical synthesis
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Pyrimidines / chemistry*
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Pyrimidines / pharmacokinetics
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Rats
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Structure-Activity Relationship
Substances
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Antihypertensive Agents
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Enzyme Inhibitors
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Phosphodiesterase 5 Inhibitors
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Pyrimidines
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Cyclic Nucleotide Phosphodiesterases, Type 5