Design, synthesis and biological evaluation of new arylpiperazine derivatives bearing a flavone moiety as α1-adrenoceptor antagonists

Bioorg Med Chem Lett. 2011 Feb 1;21(3):909-11. doi: 10.1016/j.bmcl.2010.12.080. Epub 2010 Dec 21.

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).

MeSH terms

  • Adrenergic alpha-1 Receptor Antagonists / chemical synthesis*
  • Adrenergic alpha-1 Receptor Antagonists / chemistry
  • Adrenergic alpha-1 Receptor Antagonists / pharmacology
  • Drug Design
  • Flavones / chemistry*
  • Piperazines / chemical synthesis
  • Piperazines / chemistry*
  • Piperazines / pharmacology
  • Receptors, Adrenergic, alpha-1 / chemistry*
  • Receptors, Adrenergic, alpha-1 / metabolism
  • Structure-Activity Relationship

Substances

  • Adrenergic alpha-1 Receptor Antagonists
  • Flavones
  • Piperazines
  • Receptors, Adrenergic, alpha-1
  • flavone