The discovery of potent blockers of the canonical transient receptor channels, TRPC3 and TRPC6, based on an anilino-thiazole pharmacophore

Bioorganic and Medicinal Chemistry Letters

Volumn 23, Issue 17, 2013, Pages 4979-4984

  Washburn, David G ^a   Holt, Dennis A ^a   Dodson, Jason ^a   McAtee, Jeff J ^a   Terrell, Lamont R ^a   Barton, Linda ^a   Manns, Sharada ^a   Waszkiewicz, Anna ^a   Pritchard, Christina ^a   Gillie, Dan J ^a   Morrow, Dwight M ^a   Davenport, Elizabeth A ^a   Lozinskaya, Irina M ^b   Guss, Jeffrey ^a   Basilla, Jonathan B ^a   Negron, Lorena Kallal ^a   Klein, Michael ^a   Willette, Robert N ^b   Fries, Rusty E ^a   Jensen, Timothy C ^a   Xu, Xiaoping ^b   Schnackenberg, Christine G ^b   Marino, Joseph P ^a   more..

^a GLAXOSMITHKLINE   (United States)

^b Heart Failure Discovery Performance Unit   (United States)

Author keywords

Anilino thiazole 1 Oleoyl 2 acetyl glycerol; Canonical transient receptor potential channel; OAG; TRPC3; TRPC6

Indexed keywords

2 FLUORO 4 CHLOROANILINE; 2 FLUORO 4,5 METHYLENEDIOXYANILINE; 3,4 METHYLENEDIOXYANILINE; 4 METHYLANILINE; 5,6,7,8 TETRAHYDRO 1,6 NAPHTHYRIDINE; AMIDE; ANILINE DERIVATIVE; CARBACHOL; ISOQUINOLINE DERIVATIVE; PARA ANISIDINE; PIPERIDINE DERIVATIVE; POTASSIUM CHANNEL HERG; SODIUM CHANNEL NAV1.5; THIAZOLE DERIVATIVE; TRANSIENT RECEPTOR POTENTIAL CHANNEL 3; TRANSIENT RECEPTOR POTENTIAL CHANNEL 6; TRANSIENT RECEPTOR POTENTIAL CHANNEL A1; UNCLASSIFIED DRUG; VANILLOID RECEPTOR 1; VANILLOID RECEPTOR 4; VOLTAGE GATED CALCIUM CHANNEL;

ANIMAL EXPERIMENT; ARTICLE; CONTROLLED STUDY; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG DETERMINATION; DRUG EXPOSURE; DRUG SENSITIVITY; ELECTROPHYSIOLOGY; HUMAN; HUMAN CELL; NONHUMAN; OXIDATION REDUCTION POTENTIAL; PHARMACOPHORE; RAT; RECEPTOR BLOCKING; RODENT;

RODENTIA;

1-OLEOYL-2-ACETYL-GLYCEROL; ANILINO-THIAZOLE; CANONICAL TRANSIENT RECEPTOR POTENTIAL CHANNEL; OAG; TRPC3; TRPC6;

ANILINE COMPOUNDS; DIGLYCERIDES; DRUG DISCOVERY; HEK293 CELLS; HUMANS; THIAZOLES; TRPC CATION CHANNELS;

EID: 84881376529     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2013.06.047     Document Type: Article

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