Discovery of potent, soluble and orally active TRPV1 antagonists. Structure-activity relationships of a series of isoxazoles

Bioorganic and Medicinal Chemistry Letters

Volumn 21, Issue 15, 2011, Pages 4652-4657

  Ratcliffe, Paul ^a   Abernethy, Lynn ^a   Ansari, Nasrin ^b   Cameron, Ken ^a   Clarkson, Tom ^a   Dempster, Maureen ^a   Dunn, David ^b   Easson, Anna Marie ^a   Edwards, Darren ^a   Everett, Katy ^a   Feilden, Helen ^a   Ho, Koc Kan ^b   Kultgen, Steve ^b   Littlewood, Peter ^a   MacLean, John ^a   McArthur, Duncan ^a   McGregor, Deborah ^a   McLuskey, Hazel ^a   Neagu, Irina ^b   Nimz, Olaf ^a   Nisbet, Lesley Anne ^a   Ohlmeyer, Michael ^b   Palin, Ronnie ^a   Pham, Quynhchi ^b   Rong, Yajing ^b   Roughton, Andrew ^b   Sammons, Melanie ^a   Swanson, Robert ^b   Tracey, Heather ^a   Walker, Glenn ^a   more..

^a MERCK RESEARCH LABORATORIES   (United States)

^b PHARMACOPEIA INC   (United States)

Author keywords

Antihyperalgesia; Isoxazoles; TRPV1 antagonist

Indexed keywords

4 BROMO N CYCLOPENTYL 5 (4 (TRIFLUOROMETHYL)PHENYL ISOXAZOLE 3 CARBOXAMIDE; CAPSAICIN; ISOXAZOLE DERIVATIVE; UNCLASSIFIED DRUG; VANILLOID RECEPTOR 1 ANTAGONIST;

ANALGESIC ACTIVITY; ANIMAL EXPERIMENT; ARTICLE; CONTROLLED STUDY; DRUG EFFICACY; DRUG POTENCY; DRUG SOLUBILITY; DRUG SYNTHESIS; FEMALE; NONHUMAN; PHYSICAL CHEMISTRY; RAT; STRUCTURE ACTIVITY RELATION;

ADMINISTRATION, ORAL; AMIDES; ANIMALS; CAPSAICIN; CYCLOHEXANOLS; DISEASE MODELS, ANIMAL; DRUG EVALUATION, PRECLINICAL; HUMANS; HYPERALGESIA; ISOXAZOLES; MICROSOMES, LIVER; RATS; STRUCTURE-ACTIVITY RELATIONSHIP; TRPV CATION CHANNELS;

RATTUS;

EID: 79960371480     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2011.01.051     Document Type: Article

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