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The discovery of the benzazepine class of histamine H3 receptor antagonists.
- Source :
-
Bioorganic & Medicinal Chemistry Letters . Dec2013, Vol. 23 Issue 24, p6897-6901. 5p. - Publication Year :
- 2013
-
Abstract
- 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. [Copyright &y& Elsevier]
Details
- Language :
- English
- ISSN :
- 0960894X
- Volume :
- 23
- Issue :
- 24
- Database :
- Academic Search Index
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Publication Type :
- Academic Journal
- Accession number :
- 92641349
- Full Text :
- https://doi.org/10.1016/j.bmcl.2013.09.089