• DOI:10.1016/j.bmcl.2013.09.092
Corpus ID: 20929885

The design of a novel series of muscarinic receptor antagonists leading to AZD8683, a potential inhaled treatment for COPD.

@article{Mete2013TheDO,
  title={The design of a novel series of muscarinic receptor antagonists leading to AZD8683, a potential inhaled treatment for COPD.},
  author={A. Mete and K. Bowers and R. Bull and H. Coope and D. Donald and K. J. Escott and R. Ford and K. Grime and A. Mather and Nicholas C Ray and V. Russell},
  journal={Bioorganic & medicinal chemistry letters},
  year={2013},
  volume={23 23},
  pages={
          6248-53
        }
}

• A. Mete, K. Bowers, +8 authors V. Russell
• Published 2013
• Chemistry, Medicine
• Bioorganic & medicinal chemistry letters

A novel series of muscarinic receptor antagonists was developed, with the aim of identifying a compound with high M3 receptor potency and a reduced risk of dose-limiting side effects with potential for the treatment of COPD. Initial compound modifications led to a novel cycloheptyl series, which was improved by focusing on a quinuclidine sub-series. A wide range of N-substituents was evaluated to determine the optimal substituent providing a high M3 receptor potency, high intrinsic clearance… Expand

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