The discovery of aminopyrazines as novel, potent Na v1.7 antagonists: Hit-to-lead identification and SAR

Bioorganic and Medicinal Chemistry Letters

Volumn 22, Issue 5, 2012, Pages 2033-2042

  Bregman, Howard ^a   Nguyen, Hanh Nho ^a   Feric, Elma ^a   Ligutti, Joseph ^a   Liu, Dong ^a   McDermott, Jeff S ^a   Wilenkin, Ben ^a   Zou, Anruo ^a   Huang, Liyue ^b   Li, Xingwen ^b   McDonough, Stefan I ^a   Dimauro, Erin F ^a  

^a AMGEN INC   (United States)

^b Department of Pharmacokinetics and Drug Metabolism ^*  (United States)

Author keywords

Aminopyrazine; Analgesia; Na v1.7; Sodium channels

Indexed keywords

AMINOPYRAZINE DERIVATIVE; DOFETILIDE; POTASSIUM CHANNEL HERG; PYRAZINE DERIVATIVE; SODIUM CHANNEL NAV1.7; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL EXPERIMENT; ARTICLE; DRUG CLEARANCE; DRUG POTENCY; DRUG STRUCTURE; IN VITRO STUDY; IN VIVO STUDY; LIVER MICROSOME; NONHUMAN; PROTEIN BINDING; RAT; STRUCTURE ACTIVITY RELATION;

AMINES; ANIMALS; DRUG DISCOVERY; INHIBITORY CONCENTRATION 50; MALE; PLASMA; PYRAZINES; RATS; RATS, SPRAGUE-DAWLEY; SODIUM CHANNEL BLOCKERS; SODIUM CHANNELS; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84862823467     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2012.01.023     Document Type: Article

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