The discovery and synthesis of potent zwitterionic inhibitors of renin

Bioorganic and Medicinal Chemistry Letters

Volumn 21, Issue 8, 2011, Pages 2430-2436

  Aspiotis, Renee ^a   Chen, Austin ^a   Cauchon, Elizabeth ^a   Dubé, Daniel ^a   Falgueyret, Jean Pierre ^a   Gagné, Sébastien ^a   Gallant, Michel ^a   Grimm, Erich L ^a   Houle, Robert ^a   Juteau, Hélne ^a   Lacombe, Patrick ^a   Laliberté, Sébastien ^a   Lévesque, Jean Franois ^a   MacDonald, Dwight ^a   McKay, Dan ^a   Percival, M David ^a   Roy, Patrick ^a   Soisson, Stephen M ^b   Wu, Tom ^a  

^a MERCK FROSST CENTRE FOR THERAPEUTIC RESEARCH   (Canada)

^b MERCK RESEARCH LABORATORIES   (United States)

Author keywords

CYP3A4; hERG; Hypertension; Piperidine; Renin; Zwitterion

Indexed keywords

ALISKIREN; AMPHOLYTE; ANTIHYPERTENSIVE AGENT; CYTOCHROME P450 3A4; PIPERIDINE DERIVATIVE; POTASSIUM CHANNEL HERG; PRODRUG; RENIN; RENIN INHIBITOR;

ANIMAL EXPERIMENT; ANIMAL TISSUE; AREA UNDER THE CURVE; ARTICLE; BINDING AFFINITY; DOG; DRUG BIOAVAILABILITY; DRUG DESIGN; DRUG MECHANISM; DRUG SYNTHESIS; ENZYME INHIBITION; HUMAN; HUMAN TISSUE; IC 50; NONHUMAN; RAT; RHESUS MONKEY; STRUCTURE ACTIVITY RELATION;

ADMINISTRATION, ORAL; ANIMALS; CATALYTIC DOMAIN; COMPUTER SIMULATION; DOGS; DRUG EVALUATION, PRECLINICAL; HUMANS; PIPERIDINES; PROTEASE INHIBITORS; RATS; RATS, SPRAGUE-DAWLEY; RENIN; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 79953291231     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2011.02.067     Document Type: Article

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