Discovery and optimization of aminopyrimidinones as potent and state-dependent Nav1.7 antagonists

Bioorganic and Medicinal Chemistry Letters

Volumn 22, Issue 2, 2012, Pages 1055-1060

  Nguyen, Hanh Nho ^a   Bregman, Howie ^a   Buchanan, John L ^a   Du, Bingfan ^a   Feric, Elma ^a   Huang, Liyue ^a   Li, Xingwen ^a   Ligutti, Joseph ^a   Liu, Dong ^a   Malmberg, Annika B ^a   Matson, David J ^a   McDermott, Jeff S ^a   Patel, Vinod F ^a,b   Wilenkin, Ben ^a   Zou, Anruo ^a   McDonough, Stefan I ^a   Dimauro, Erin F ^a  

^a AMGEN INC   (United States)

^b Sanofi Aventis   (United States)

Author keywords

Aminopyrimidinone; Congenital indifference to pain; Nav channels; Nav1.7; Paroxysmal extreme pain disorder; Primary erythromelalgia; Sodium channel antagonists; Sodium channel blockers; Sodium channel inhibitors; Voltage gated sodium channels

Indexed keywords

AMINOPYRIMIDINONE DERIVATIVE; N ME AMINOPYRIMIDINONE; POTASSIUM CHANNEL HERG; SODIUM CHANNEL BLOCKING AGENT; SODIUM CHANNEL NAV1.7; UNCLASSIFIED DRUG;

ANIMAL CELL; ARTICLE; DRUG CLEARANCE; DRUG DISTRIBUTION; ELECTROPHYSIOLOGY; IC 50; MALE; NONHUMAN; RAT; STRUCTURE ACTIVITY RELATION;

ANIMALS; DOSE-RESPONSE RELATIONSHIP, DRUG; HUMANS; LIGANDS; MICROSOMES, LIVER; MOLECULAR STRUCTURE; PYRIMIDINONES; RATS; SODIUM CHANNELS; STRUCTURE-ACTIVITY RELATIONSHIP;

RATTUS;

EID: 84855657020     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2011.11.111     Document Type: Article

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