1,4-Dioxane, a suitable scaffold for the development of novel M3 muscarinic receptor antagonists

Fabio Del Bello, Elisabetta Barocelli, Simona Bertoni, Alessandro Bonifazi, Mercedes Camalli, Gaetano Campi, Mario Giannella, Rosanna Matucci, Marta Nesi, Maria Pigini, Wilma Quaglia, Alessandro Piergentili

Research output: Contribution to journalArticlepeer-review

23 Scopus citations

Abstract

In this study the modulation of the pharmacological profile from agonist to antagonist was successfully obtained by replacing the methyl group in position 6 of the 1,4-dioxane scaffold of the potent M2/M3 muscarinic agonist 1 with bulkier groups. In particular, the 6,6-diphenyl substitution provided the potent M3 preferring antagonist (±)-17, which in in vivo study proved to be effective in reducing the volume-induced contractions of rat urinary bladder and was devoid of cardiovascular effects.

Original languageEnglish (US)
Pages (from-to)1783-1787
Number of pages5
JournalJournal of medicinal chemistry
Volume55
Issue number4
DOIs
StatePublished - Feb 23 2012
Externally publishedYes

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

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