2. Academic Validation
  3. Novel benzothiophene H1-antihistamines for the treatment of insomnia

Novel benzothiophene H1-antihistamines for the treatment of insomnia

  • Bioorg Med Chem Lett. 2010 Apr 1;20(7):2316-20. doi: 10.1016/j.bmcl.2010.01.134.
Wilna J Moree 1,  Florence Jovic,  Timothy Coon,  Jinghua Yu,  Bin-Feng Li,  Fabio C Tucci,  Dragan Marinkovic,  Raymond S Gross,  Siobhan Malany,  Margaret J Bradbury,  Lisa M Hernandez,  Zhihong O'Brien,  Jianyun Wen,  Hua Wang,  Samuel R J Hoare,  Robert E Petroski,  Aida Sacaan,  Ajay Madan,  Paul D Crowe,  Graham Beaton
Affiliations

Affiliation

  • 1 Neurocrine Biosciences, 12780 El Camino Real, San Diego, CA 92130, USA. wilna.moree@gmail.com
PMID: 20188547 DOI: 10.1016/j.bmcl.2010.01.134
Abstract

SAR of lead benzothiophene H(1)-antihistamine 2 was explored to identify backup candidates with suitable pharmacokinetic profiles for an insomnia program. Several potent and selective H(1)-antihistamines with a range of projected half-lives in humans were identified. Compound 16d had a suitable human half-life as demonstrated in a human microdose study, but variability in pharmacokinetic profile, attributed to metabolic clearance, prevented further development of this compound. Compound 28b demonstrated lower predicted clearance in preclinical studies, and may represent a more suitable backup compound.

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