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2000
Volume 10, Issue 4
  • ISSN: 1573-4064
  • E-ISSN: 1875-6638

Abstract

Previous structure-activity relationship studies involving a series of lactone-based muscarinic ligands identified a lead compound containing a diphenylmethylpiperazine moiety (4; IC50 = 340 nM). The purpose of the present work is to investigate 1,3-benzodioxoles, 4,4-diethyl substituted tetrahydrofurans, 5-substituted oxazolidinones and chromones as bioisosteric replacements for the lactone ring in a novel series of muscarinic ligands. The approach provided compounds with improved % inhibition values and identified a non-selective muscarinic ligand with an IC50 value of 280 nM. The structure-activity relationship for this new series will be discussed. Selected compounds were evaluated in preliminary assays for subtype selectivity and were found to be non-selective.

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/content/journals/mc/10.2174/15734064113096660043
2014-06-01
2025-06-09
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  • Article Type:
    Research Article
Keyword(s): 1; 3-benzodioxole; Bioisostere; chromones; oxazolidinone; tetrahydrofuran
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