Discovery of substituted lactams as novel dual orexin receptor antagonists. Synthesis, preliminary structure-activity relationship studies and efforts towards improved metabolic stability and pharmacokinetic properties. Part 1

Bioorganic and Medicinal Chemistry Letters

Volumn 24, Issue 4, 2014, Pages 1201-1208

  Sifferlen, Thierry ^a   Boller, Amandine ^a   Chardonneau, Audrey ^a   Cottreel, Emmanuelle ^a   Hoecker, Johannes ^a   Aissaoui, Hamed ^a   Williams, Jodi T ^a   Brotschi, Christine ^a   Heidmann, Bibia ^a   Siegrist, Romain ^a   Gatfield, John ^a   Treiber, Alexander ^a   Brisbare Roch, Catherine ^a   Jenck, Francois ^a   Boss, Christoph ^a  

^a ACTELION PHARMACEUTICALS LTD   (Switzerland)

Author keywords

CNS drug discovery; G protein coupled receptors; Metabolic stability; Orexin antagonists; Structure activity relationship studies

Indexed keywords

CNS DRUG DISCOVERY; G-PROTEIN COUPLED RECEPTORS; METABOLIC STABILITY; OREXIN ANTAGONISTS; STRUCTURE-ACTIVITY RELATIONSHIP STUDIES;

ANIMALS; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG DISCOVERY; HUMANS; LACTAMS; MOLECULAR STRUCTURE; OREXIN RECEPTORS; RATS; RATS, WISTAR; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84893721035     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2013.12.092     Document Type: Article

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