Abstract
A 4-centre PDE4 pharmacophore search has been carried out in several 3D-databases containing compounds belonging to different therapeutic areas. Losartan, an angiotensin-II antagonist, has been identified as a new lead compound for developing PDE4 inhibitors. New families of compounds derived from losartan has been synthesized and their PDE inhibition has been measured.
MeSH terms
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Animals
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Drug Design
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Guinea Pigs
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Heart Ventricles / drug effects
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Heart Ventricles / enzymology
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In Vitro Techniques
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Losartan / chemistry
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Losartan / pharmacology*
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Phosphodiesterase Inhibitors / chemical synthesis
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Phosphodiesterase Inhibitors / chemistry
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Phosphodiesterase Inhibitors / pharmacology*
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Structure-Activity Relationship
Substances
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Phosphodiesterase Inhibitors
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Losartan