Design, synthesis and structure-activity relationships of (indo-3-yl) heterocyclic derivatives as agonists of the CB1 receptor. Discovery of a clinical candidate

Bioorganic and Medicinal Chemistry Letters

Volumn 21, Issue 8, 2011, Pages 2541-2546

  Ratcliffe, Paul ^a   Adam, Julia M ^a   Baker, James ^a   Bursi, Roberta ^b   Campbell, Robert ^a   Clark, John K ^a   Cottney, Jean E ^a   Deehan, Maureen ^a   Easson, Anna Marie ^a   Ecker, Daniel ^c   Edwards, Darren ^a   Epemolu, Ola ^a   Evans, Louise ^a   Fields, Ruth ^a   Francis, Stuart ^a   Harradine, Paul ^a   Jeremiah, Fiona ^a   Kiyoi, Takao ^a   McArthur, Duncan ^a   Morrison, Angus ^a   Passier, Paul ^b   Pick, Jack ^a   Schnabel, Peter G ^c,d   Schulz, Jurgen ^a   Steinbrede, Heinz ^c   Walker, Glenn ^a   Westwood, Paul ^a   Wishart, Grant ^a   Haes, Joanna Udo De ^b   more..

^a MERCK RESEARCH LABORATORIES   (United States)

^b MSD   (Netherlands)

^c Profil Institut fur Stoffwechselforschung GmbH   (Germany)

^d FOCUS   (Germany)

Author keywords

Cannabinoid; CB1 receptor agonist; Clinical candidate; GPCR

Indexed keywords

CANNABINOID 1 RECEPTOR; CANNABINOID 1 RECEPTOR AGONIST; G PROTEIN COUPLED RECEPTOR; HETEROCYCLIC COMPOUND; INDOLE DERIVATIVE; POTASSIUM CHANNEL HERG; THIAZOLE DERIVATIVE;

ANALGESIC ACTIVITY; ANIMAL CELL; ARTICLE; CLINICAL EFFECTIVENESS; DRUG CLEARANCE; DRUG DESIGN; DRUG HALF LIFE; DRUG METABOLISM; DRUG POTENCY; DRUG SOLUBILITY; DRUG STRUCTURE; DRUG SYNTHESIS; HUMAN; HUMAN CELL; NONHUMAN; STRUCTURE ACTIVITY RELATION; TAIL FLICK TEST;

ANIMALS; CYTOCHROME P-450 ENZYME SYSTEM; DOGS; DRUG DESIGN; DRUG EVALUATION, PRECLINICAL; HETEROCYCLIC COMPOUNDS; INDOLES; MICE; RATS; RATS, WISTAR; RECEPTOR, CANNABINOID, CB1; STRUCTURE-ACTIVITY RELATIONSHIP; THIAZOLES;

EID: 79953282219     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2011.02.023     Document Type: Article

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