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Bioorg Med Chem Lett. 2009 Aug 15;19(16):4747-51. doi: 10.1016/j.bmcl.2009.06.059. Epub 2009 Jun 17.

Synthesis and SAR studies of 1,4-diazabicyclo[3.2.2]nonane phenyl carbamates--subtype selective, high affinity alpha7 nicotinic acetylcholine receptor agonists.

Author information

1
Neuroscience Medicinal Chemistry, Pfizer Global Research & Development, Groton, CT 06340, United States. christopher.j.odonnell@pfizer.com

Abstract

The synthesis and SAR studies about the bicyclic amine, carbamate linker and aromatic ring of a 1,4-diazabicyclo[3.2.2]nonane phenyl carbamate series of alpha7 nAChR agonists is described. The development of the medicinal chemistry strategy and SAR which led to the identification of 5 and 7aa as subtype selective, high affinity alpha7 agonists as excellent leads for further evaluation is discussed, along with key physicochemical and pharmacokinetic data highlighting their lead potential.

PMID:
19576766
DOI:
10.1016/j.bmcl.2009.06.059
[Indexed for MEDLINE]

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