Moree, Wilna J.; Jovic, Florence; Coon, Timothy; Yu, Jinghua; Li, Bin-Feng; Tucci, Fabio C.; Marinkovic, Dragan; Gross, Raymond S.; Malany, Siobhan; Bradbury, Margaret J.; Hernandez, Lisa M.; O’Brien, Zhihong; Wen, Jianyun; Wang, Hua; Hoare, Samuel R. J.; Petroski, Robert E.; Sacaan, Aida; Madan, Ajay; Crowe, Paul D.; Beaton, Graham published the artcile< Novel benzothiophene H1-antihistamines for the treatment of insomnia>, Computed Properties of 1003-32-3, the main research area is benzothiophene preparation H1 antihistamine treatment insomnia.
SAR of lead benzothiophene H1-antihistamine I (R = 2-pyridyl) was explored to identify backup candidates with suitable pharmacokinetic profiles for an insomnia program. Several potent and selective H1-antihistamines with a range of projected half-lives in humans were identified. 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 I (R = 1-pyrazolyl) demonstrated lower predicted clearance in preclin. studies, and may represent a more suitable backup compound
Bioorganic & Medicinal Chemistry Letters published new progress about Histamine H1 receptor antagonists. 1003-32-3 belongs to class thiazole, and the molecular formula is C4H3NOS, Computed Properties of 1003-32-3.
Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica