التفاصيل البيبلوغرافية
العنوان:
Discovery of 1 H -pyrazolo[3,4- b ]pyridines as potent dual orexin receptor antagonists (DORAs)
المؤلفون:
Arndt Meyer , Murali Chebrolu , Christine E. Gee , Grit Laue , Markus Fendt , Laura H. Jacobson , Sangamesh Badiger , Samuel Hintermann , Chetan Pandit , Simona Cotesta , Claudia Betschart , Daniel Hoyer , Vinod D. Chaudhari , Dirk Behnke , Trixie Wagner
المصدر:
Bioorganic & Medicinal Chemistry Letters . 25:5555-5560
بيانات النشر:
Elsevier BV, 2015.
سنة النشر:
2015
مصطلحات موضوعية:
Pyridines , High-throughput screening , Clinical Biochemistry , Dual Orexin Receptor Antagonists , Administration, Oral , Pharmaceutical Science , Pharmacology , Crystallography, X-Ray , Doras , Biochemistry , Mice , Drug Discovery , Animals , Molecular Biology , G protein-coupled receptor , Molecular Structure , biology , Chemistry , Drug discovery , Orexin Receptor Antagonists , Organic Chemistry , biology.organism_classification , Orexin , Pyrazoles , Molecular Medicine , Administration, Intravenous , Protein Binding
الوصف:
Compound rac-1 was identified by high throughput screening. Here we report SAR studies and MedChem optimization towards the highly potent dual orexin receptor antagonists (S)-2 and (S)-3. Furthermore, strategies to overcome the suboptimal physicochemical properties are highlighted and the pharmacokinetic profiles of representative compounds is presented.
تدمد:
0960-894X
URL الوصول:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::683f840d5741ac67440ee89e98efc728 https://doi.org/10.1016/j.bmcl.2015.10.055
حقوق:
CLOSED
رقم الأكسشن:
edsair.doi.dedup.....683f840d5741ac67440ee89e98efc728
قاعدة البيانات:
OpenAIRE
