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Bioorg Med Chem Lett. 2013 Dec 15;23(24):6897-901. doi: 10.1016/j.bmcl.2013.09.089. Epub 2013 Oct 5.

The discovery of the benzazepine class of histamine H3 receptor antagonists.

Author information

1
GlaxoSmithKline R&D, Neurology CEDD, Harlow, Essex CM19 5AW, United Kingdom. Electronic address: David.M.Wilson@astrazeneca.com.

Abstract

This Letter describes the discovery of a novel series of H3 receptor antagonists. The initial medicinal chemistry strategy focused on deconstructing and simplifying an early screening hit which rapidly led to the discovery of a novel series of H3 receptor antagonists based on the benzazepine core. Employing an H3 driven pharmacodynamic model, the series was then further optimised through to a lead compound that showed robust in vivo functional activity and possessed overall excellent developability properties.

KEYWORDS:

Alzheimer’s disease; Benzazepine; GPCR; H(3) receptor antagonist; Histamine; Neurotransmitters

PMID:
24161834
DOI:
10.1016/j.bmcl.2013.09.089
[Indexed for MEDLINE]

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