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Design, synthesis and structure–activity relationship of N-substituted tropane muscarinic acetylcholine receptor antagonists

Authors
Journal
Bioorganic & Medicinal Chemistry Letters
0960-894X
Publisher
Elsevier
Publication Date
Volume
22
Issue
9
Identifiers
DOI: 10.1016/j.bmcl.2012.02.015
Keywords
  • Inhaled
  • Muscarinic Antagonist
  • Copd
  • Tropane
  • Quaternary Ammonium Salts

Abstract

Abstract A novel series of N-substituted tropane derivatives was characterized as potent muscarinic acetylcholine receptor antagonists (mAChRs). Kinetic washout studies showed that the N-endosubstituted analog 24 displayed much slower reversibility at mAChRs than the methyl-substituted parent molecule darotropium. In addition, it was shown that this characteristic appeared to translate into enhanced which duration of action in a mouse model of bronchonstriction.

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