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, highl
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Discovery and characterization of vicriviroc (SCH 417690), a CCR5 antagonist with potent activity against human immunodeficiency virus type 1Potent antiviral synergy between monoclonal antibody and small-molecule CCR5 inhibitors of human immunodeficiency virus type 1Two HIV-1 variants resistant to small molecule CCR5 inhibitors differ in how they use CCR5 for entryPharmacokinetic/pharmacodynamic modeling of the antiretroviral activity of the CCR5 antagonist Vicriviroc in treatment experienced HIV-infected subjects (ACTG protocol 5211).Anibamine, a natural product CCR5 antagonist, as a novel lead for the development of anti-prostate cancer agentsMaraviroc (UK-427,857), a potent, orally bioavailable, and selective small-molecule inhibitor of chemokine receptor CCR5 with broad-spectrum anti-human immunodeficiency virus type 1 activity.CCR5 antagonists: host-targeted antivirals for the treatment of HIV infection.Structural Analysis of Chemokine Receptor-Ligand Interactions.HIV entry inhibitors and their potential in HIV therapyRegio- and stereoselective syntheses of the natural product CCR5 antagonist anibamine and its three olefin isomers.Development of anti-HIV peptides based on a viral capsid protein.Cell surface expression of CCR5 and other host factors influence the inhibition of HIV-1 infection of human lymphocytes by CCR5 ligands.Oral CCR5 inhibitors: will they make it through?The road map to oral bioavailability: an industrial perspective.Involvement of the second extracellular loop and transmembrane residues of CCR5 in inhibitor binding and HIV-1 fusion: insights into the mechanism of allosteric inhibition.Human Immunodeficiency Virus Immune Cell Receptors, Coreceptors, and Cofactors: Implications for Prevention and Treatment.Tissue-specific sequence alterations in the human immunodeficiency virus type 1 envelope favoring CCR5 usage contribute to persistence of dual-tropic virus in the brain.Pharmacotherapy of HIV-1 Infection: Focus on CCR5 Antagonist Maraviroc.International Union of Basic and Clinical Pharmacology. [corrected]. LXXXIX. Update on the extended family of chemokine receptors and introducing a new nomenclature for atypical chemokine receptors.Chemokine receptor antagonists: part 2.CCR5 antagonists: the answer to inflammatory disease?Novel CCR5 antagonists for the treatment of HIV infection: a review of compounds patented in 2006 - 2008.Vicriviroc, a new CC-chemokine receptor 5 inhibitor for treatment of HIV: properties, promises and challenges.Small molecule HIV entry inhibitors: Part I. Chemokine receptor antagonists: 2004 - 2010.Conformational HIV-1 envelope on particulate structures: a tool for chemokine coreceptor binding studies.CCR5 inhibitors: emergence, success, and challenges.The successes and failures of HIV drug discovery.Targeting CCR5 for anti-HIV research.Incorporation of Privileged Structures into Bevirimat Can Improve Activity against Wild-Type and Bevirimat-Resistant HIV-1.CCR5 receptor antagonists in preclinical to phase II clinical development for treatment of HIV.Discovery of INCB9471, a Potent, Selective, and Orally Bioavailable CCR5 Antagonist with Potent Anti-HIV-1 Activity4-Azatricyclo[5.2.2.02,6]undecane-3,5,8-triones as potential pharmacological agents.Comparative docking study of anibamine as the first natural product CCR5 antagonist in CCR5 homology models.Development of a Moloney murine leukemia virus-based pseudotype anti-HIV assay suitable for accurate and rapid evaluation of HIV entry inhibitors.Development of a novel dual CCR5-dependent and CXCR4-dependent cell-cell fusion assay system with inducible gp160 expression.Synthesis of (3) H, (2) H4 and (14) C-SCH 417690 (Vicriviroc).A simple structure-based model for the prediction of HIV-1 co-receptor tropism.HIV-1 clones resistant to a small molecule CCR5 inhibitor use the inhibitor-bound form of CCR5 for entry.The Expanding Therapeutic Perspective of CCR5 Blockade.
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P2860
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, highl
description
2004 nî lūn-bûn
@nan
2004 թուականի Մայիսին հրատարակուած գիտական յօդուած
@hyw
2004 թվականի մայիսին հրատարակված գիտական հոդված
@hy
2004年の論文
@ja
2004年論文
@yue
2004年論文
@zh-hant
2004年論文
@zh-hk
2004年論文
@zh-mo
2004年論文
@zh-tw
2004年论文
@wuu
name
Piperazine-based CCR5 antagoni ...... 417690/Sch-D), a potent, highl
@nl
type
label
Piperazine-based CCR5 antagoni ...... 417690/Sch-D), a potent, highl
@nl
prefLabel
Piperazine-based CCR5 antagoni ...... 417690/Sch-D), a potent, highl
@nl
P2093
P356
P1476
Piperazine-based CCR5 antagoni ...... y bioavailable CCR5 antagonist
@en
P2093
Bahige M Baroudy
Dennis Nazareno
Geoffrey Varty
Jayaram R Tagat
Jean Lachowicz
Julie M Strizki
Kathleen Cox
Marc A Labroli
Robert Watkins
Ruo W Steensma
P304
P356
10.1021/JM0304515
P407
P577
2004-05-06T00:00:00Z