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J Med Chem. 2009 Sep 10;52(17):5323-9. doi: 10.1021/jm9008218.

Discovery of orally active 3-pyridinyl-tropane as a potent nociceptin receptor agonist for the management of cough.

Author information

1
Department of Chemical Research-CV & CNS, Schering-Plough Research Institute, Kenilworth, New Jersey 07033, USA. shu-wei.yang@spcorp.com

Abstract

A series of 3-pyridinyl-tropane analogues based on previously reported compound 1 have been synthesized and shown to bind to the nociceptin receptor with high affinity. From the SAR study and our lead optimization efforts, compound 10 was found to possess potent oral antitussive activity in the capsaicin-induced guinea pig model. The rationale for compound selection and the biological profile of the optimized lead (10) are disclosed.

PMID:
19678644
DOI:
10.1021/jm9008218
[Indexed for MEDLINE]

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