The design and synthesis of novel, phosphonate-containing transient receptor potential melastatin 8 (TRPM8) antagonists

Bioorganic and Medicinal Chemistry Letters

Volumn 22, Issue 8, 2012, Pages 2922-2926

  Matthews, Jay M ^a   Qin, Ning ^b   Colburn, Raymond W ^c   Dax, Scott L ^d   Hawkins, Mike ^e   McNally, James J ^a   Reany, Laura ^c   Youngman, Mark A ^f   Baker, Judith ^c   Hutchinson, Tasha ^g   Liu, Yi ^a   Lubin, Mary Lou ^h   Neeper, Michael ^a   Brandt, Michael R ^c   Stone, Dennis J ^c   Flores, Christopher M ^a  

^a J/Johnson Pharmaceut Res/Devmt   (United States)

^b Roche R and D Ltd   (China)

^c JOHNSON AND JOHNSON   (United States)

^d Galleon Pharmaceuticals   (United States)

^e TREVENA INC   (United States)

^f PURDUE PHARMA L P   (United States)

^g PhaseBio Pharmaceuticals Inc   (United States)

^h MERCK RESEARCH LABORATORIES   (United States)

Author keywords

Cold allodynia; Cold menthol receptor (CMR1); Melostatin 8; Transient receptor potential; TRPM8

Indexed keywords

1 (2 HYDROXYPHENYL) 4 (3 NITROPHENYL) 1,2,3,6 TETRAHYDROPYRIMIDIN 2 ONE; AROMATIC COMPOUND; BENZOTHIOPHENE DERIVATIVE; CHEMICAL AGENT; PHOSPHONIC ACID DERIVATIVE; RECEPTOR BLOCKING AGENT; TRANSIENT RECEPTOR POTENTIAL CHANNEL M8; TRANSIENT RECEPTOR POTENTIAL MELASTATIN 8 ANTAGONIST; UNCLASSIFIED DRUG;

ARTICLE; ASSAY; CHEMICAL MODIFICATION; DRUG DESIGN; DRUG POTENCY; DRUG SELECTIVITY; DRUG SYNTHESIS; FLUOROMETRIC IMAGING PLATE READER ASSAY; HUMAN; NONHUMAN; RAT; STEREOSPECIFICITY; STRUCTURE ACTIVITY RELATION; WET DOG SHAKES;

ANIMALS; CELL LINE; CHROMATOGRAPHY, HIGH PRESSURE LIQUID; DOGS; DRUG DESIGN; INHIBITORY CONCENTRATION 50; MOLECULAR STRUCTURE; PHOSPHONIC ACIDS; PROTEIN BINDING; RATS; STRUCTURE-ACTIVITY RELATIONSHIP; TRPM CATION CHANNELS;

CANIS FAMILIARIS; RATTUS;

EID: 84862776608     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2012.02.060     Document Type: Article

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