Isosteric replacements for benzothiazoles and optimisation to potent Cathepsin K inhibitors free from hERG channel inhibition

Bioorganic and Medicinal Chemistry Letters

Volumn 22, Issue 17, 2012, Pages 5563-5568

  Dossetter, Alexander G ^a   Bowyer, Jonathan ^a   Cook, Calum R ^a   Crawford, James J ^a   Finlayson, Jonathan E ^a   Heron, Nicola M ^a   Heyes, Christine ^a   Highton, Adrian J ^a   Hudson, Julian A ^a   Jestel, Anja ^b   Krapp, Stephan ^b   MacFaul, Philip A ^a   McGuire, Thomas M ^a   Morley, Andrew D ^a   Morris, Jeffrey J ^a   Page, Ken M ^a   Ribeiro, Lyn Rosenbrier ^a   Sawney, Helen ^a   Steinbacher, Stefan ^b   Smith, Caroline ^a  

^a ASTRAZENECA   (United Kingdom)

^b PROTEROS BIOSTRUCTURES GMBH   (Germany)

Author keywords

Cathepsin K; Covalent inhibitor; hERG; Matched molecular pair analysis; MMPA; Molecular complexity; Pharmacokinetics; Structure based design; Synthesis

Indexed keywords

BENZOTHIAZOLE; CATHEPSIN K INHIBITOR; NITRILE; POTASSIUM CHANNEL HERG;

ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; DRUG BIOAVAILABILITY; IN VIVO STUDY; NONHUMAN; RAT;

ANIMALS; BENZOTHIAZOLES; CATHEPSIN K; DOGS; ETHER-A-GO-GO POTASSIUM CHANNELS; HUMANS; MICROSOMES, LIVER; MODELS, MOLECULAR; NITRILES; RATS; STRUCTURE-ACTIVITY RELATIONSHIP;

CANIS FAMILIARIS;

EID: 84865148233     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2012.07.012     Document Type: Article

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