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Bioorganic and Medicinal Chemistry Letters

Volumn 22, Issue 5, 2012, Pages 2052-2062

Discovery and hit-to-lead optimization of pyrrolopyrimidines as potent, state-dependent Na v1.7 antagonists

(12) Chakka, Nagasree a Bregman, Howie a Du, Bingfan a Nguyen, Hanh Nho a Buchanan, John L a Feric, Elma a Ligutti, Joseph a Liu, Dong a McDermott, Jeff S a Zou, Anruo a McDonough, Stefan I a Dimauro, Erin F a

a AMGEN INC (United States)

Author keywords

Congenital indifference to pain; Na v channels; Na v1.7; Paroxysmal extreme pain disorder; Primary erythromelalgia; Pyrrolopyrimidine; Sodium channel antagonists; Sodium channel blockers; Sodium channel inhibitors; Voltage gated sodium channels

Indexed keywords

METHYL GROUP; POTASSIUM CHANNEL HERG; PYRAZOLOPYRIMIDINE DERIVATIVE; PYRROLOPYRIMIDINE DERIVATIVE; SODIUM CHANNEL NAV1.7;

ARTICLE; DRUG POTENCY; DRUG SYNTHESIS; HUMAN; HUMAN CELL; LIPOPHILICITY; MICROSOME; MOLECULE; STRUCTURE ACTIVITY RELATION;

DRUG DISCOVERY; HUMANS; MICROSOMES, LIVER; PAIN; PYRIMIDINES; PYRROLES; SODIUM CHANNEL BLOCKERS; SODIUM CHANNELS; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84862782527 PISSN: 0960894X EISSN: 14643405 Source Type: Journal
DOI: 10.1016/j.bmcl.2012.01.015 Document Type: Article

Times cited : (27)

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