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Novel and highly selective postsynaptic α-adrenoreceptor antagonists: synthesis and structure-activity relationships of alkane-bridged [4-(phenoxyethyl)-1-piperazinyl]-3(2H)-pyridazinones

Authors
Journal
European Journal of Medicinal Chemistry
0223-5234
Publisher
Elsevier
Publication Date
Volume
30
Issue
1
Identifiers
DOI: 10.1016/0223-5234(96)88211-0
Keywords
  • Pyridazinone
  • α-Adrenoreceptor
  • α-Antagonist Structure-Activity Relationship
  • Rat Vas Deferens

Abstract

Summary The synthesis of selected 4-[4-(phenoxyethyl)-1-piperazinyl]-3(2 H)-pyridazinones and alkane-bridged dimers of 4-, 5- and 6-[4-(phenoxyethyl)-1-piperazinyl]-3(2 H)-pyridazinones is reported. The blocking activity of these compounds was determined on the pre- and postsynaptic α-adrenoreceptors of isolated rat vas deferons.

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