Piperazine-Based CCR5 Antagonists as HIV-1 Inhibitors. IV. Discovery of 1-[(4,6-Dimethyl-5-pyrimidinyl) carbonyl]-4-[4-{2-methoxy-1(R)-4-(trifluoromethyl)-phenyl}ethyl-3(S) -methyl-1-piperazinyl]-4-methylpiperidine (Sch-417690/Sch-D), a Potent, Highly Selective, and Orally Bioavailable CCR5 Antagonist

Journal of Medicinal Chemistry

Volumn 47, Issue 10, 2004, Pages 2405-2408

  Tagat, Jayaram R ^a   McCombie, Stuart W ^a   Nazareno, Dennis ^a   Labroli, Marc A ^a   Xiao, Yushi ^a   Steensma, Ruo W ^a   Strizki, Julie M ^a   Baroudy, Bahige M ^a   Cox, Kathleen ^a   Lachowicz, Jean ^a   Varty, Geoffrey ^a   Watkins, Robert ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

1 [(4,6 DIMETHYL 5 PYRIMIDINYL)CARBONYL] 4 [4 [2 METHOXY 4 (TRIFLUOROMETHYL)PHENYL]ETHYL 3 METHYL 1 PIPERAZINYL] 4 METHYLPIPERIDINE; CHEMOKINE RECEPTOR CCR5; CHEMOKINE RECEPTOR CCR5 ANTAGONIST; PIPERAZINE DERIVATIVE; UNCLASSIFIED DRUG; VICRIVIROC;

ANTIVIRAL ACTIVITY; ARTICLE; DRUG BIOAVAILABILITY; DRUG POTENCY; HUMAN IMMUNODEFICIENCY VIRUS 1; RECEPTOR AFFINITY; TARGET CELL; VIRUS ADSORPTION;

ADMINISTRATION, ORAL; ANIMALS; ANTI-HIV AGENTS; BIOLOGICAL AVAILABILITY; BRAIN; CATION TRANSPORT PROTEINS; DIGESTIVE SYSTEM; ETHER-A-GO-GO POTASSIUM CHANNELS; HIV-1; HUMANS; LEUKOCYTES, MONONUCLEAR; MACACA FASCICULARIS; PIPERAZINES; PIPERIDINES; POTASSIUM CHANNELS; POTASSIUM CHANNELS, VOLTAGE-GATED; PYRIMIDINES; RATS; RECEPTORS, CCR5; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 2342544143     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm0304515     Document Type: Article

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