Abstract
Elaborate study on the three-dimensional model of α(1)-adrenoceptor (α(1)-AR) antagonists led to the development of a series of new arylpiperazine derivatives bearing a flavone nucleus as α(1)-AR antagonists. The in vitro activities were evaluated and compounds 1, 4, 10, 13 and 15 showed activities close to the reference compound (Prazosin).
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MeSH terms
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Adrenergic alpha-1 Receptor Antagonists / chemical synthesis*
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Adrenergic alpha-1 Receptor Antagonists / chemistry
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Adrenergic alpha-1 Receptor Antagonists / pharmacology
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Drug Design
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Flavones / chemistry*
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Piperazines / chemical synthesis
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Piperazines / chemistry*
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Piperazines / pharmacology
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Receptors, Adrenergic, alpha-1 / chemistry*
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Receptors, Adrenergic, alpha-1 / metabolism
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Structure-Activity Relationship
Substances
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Adrenergic alpha-1 Receptor Antagonists
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Flavones
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Piperazines
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Receptors, Adrenergic, alpha-1
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flavone