Abstract
A novel class of dual pharmacology bronchodilators targeting both β(2)-adrenoceptor and PDE4 was designed and synthesised by combining the pharmacophores of salmeterol and roflumilast or phthalazinone. All the compounds exhibited better β(2)-adrenoceptor agonist activities (pEC(50)=8.47-9.20) than the reference compound salmeterol (pEC(50)=8.3) and good inhibitory activity on PDE4B2 (IC(50)=0.235-1.093 μM).
Copyright © 2012 Elsevier Ltd. All rights reserved.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Adrenergic beta-2 Receptor Agonists / chemistry
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Adrenergic beta-2 Receptor Agonists / pharmacology*
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Albuterol / analogs & derivatives*
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Albuterol / chemistry
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Albuterol / pharmacology
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Aminopyridines / chemistry*
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Aminopyridines / pharmacology*
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Benzamides / chemistry*
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Benzamides / pharmacology*
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Bronchodilator Agents / pharmacology
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Cyclopropanes / chemistry
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Cyclopropanes / pharmacology
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Humans
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Phosphodiesterase 4 Inhibitors / chemistry
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Phosphodiesterase 4 Inhibitors / pharmacology*
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Pulmonary Disease, Chronic Obstructive / drug therapy*
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Salmeterol Xinafoate
Substances
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Adrenergic beta-2 Receptor Agonists
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Aminopyridines
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Benzamides
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Bronchodilator Agents
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Cyclopropanes
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Phosphodiesterase 4 Inhibitors
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Roflumilast
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Salmeterol Xinafoate
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Albuterol