A potent and orally active HIV-1 integrase inhibitor

被引:24
|
作者
Egbertson, Melissa S. [1 ]
Moritz, H. Marie
Melamed, Jeffrey Y.
Han, Wei
Perlow, Debra S.
Kuo, Michelle S.
Embrey, Mark
Vacca, Joseph P.
Zrada, Matthew M.
Cortes, Amanda R.
Wallace, Audrey
Leonard, Yvonne
Hazuda, Daria J.
Miller, Michael D.
Felock, Peter J.
Stillmock, Kara A.
Witmer, Marc V.
Schleif, William
Gabryelski, Lori J.
Moyer, Gregory
Ellis, Joan D.
Jin, Lixia
Xu, Wei
Braun, Matthew P.
Kassahun, Kellem
Tsou, Nancy N.
Young, Steven D.
机构
[1] Merck Res Labs, Dept Med Chem, West Point, PA 19486 USA
[2] Merck Res Labs, Dept Biol Chem, West Point, PA 19486 USA
[3] Merck Res Labs, Dept Viral Vaccine Res, West Point, PA 19486 USA
[4] Merck Res Labs, Pharmaceut Res Dept, West Point, PA 19486 USA
[5] Merck Res Labs, Dept Drug Metab, West Point, PA 19486 USA
[6] Dept Med Chem, Rahway, NJ 07065 USA
关键词
HIV; AIDS; integrase; strand transfer; 1,6-naphthyridine;
D O I
10.1016/j.bmcl.2006.11.080
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A 1,6-naphthyridine inhibitor of HIV-1 integrase has been discovered with excellent inhibitory activity in cells, good pharmacokinetics, and an excellent ability to inhibit virus with mutant enzyme. (c) 2006 Elsevier Ltd. All rights reserved.
引用
收藏
页码:1392 / 1398
页数:7
相关论文
共 50 条
  • [31] Electrostatic Properties of Two Precursors of Potent HIV-1 Integrase Inhibitors
    Firley, Delphine
    Courcot, Blandine
    Gillet, Jean-Michel
    Spasojevic-de Bire, Anne
    Fraisse, Bernard
    Zouhiri, Fatima
    Desmaele, Didier
    d'Angelo, Jean
    Ghermani, Nour Eddine
    ACTA CRYSTALLOGRAPHICA A-FOUNDATION AND ADVANCES, 2005, 61 : C277 - C277
  • [32] Viracept (nelfinavir mesylate, AG1343): A potent, orally bioavailable inhibitor of HIV-1 protease
    Kaldor, SW
    Kalish, VJ
    Davies, JF
    Shetty, BV
    Fritz, JE
    Appelt, K
    Burgess, JA
    Campanale, KM
    Chirgadze, NY
    Clawson, DK
    Dressman, BA
    Hatch, SD
    Khalil, DA
    Kosa, MB
    Lubbehusen, PP
    Muesing, MA
    Patick, AK
    Reich, SH
    Su, KS
    Tatlock, JH
    JOURNAL OF MEDICINAL CHEMISTRY, 1997, 40 (24) : 3979 - 3985
  • [33] Raltegravir: the first HIV-1 integrase strand transfer inhibitor in the HIV armamentarium
    Nguyen, Bach-Yen T.
    Isaacs, Robin D.
    Teppler, Hedy
    Leavitt, Randi Y.
    Sklar, Peter
    Iwamoto, Marian
    Wenning, Larissa A.
    Miller, Michael D.
    Chen, Joshua
    Kemp, Ramon
    Xu, Wei
    Fromtling, Robert A.
    Vacca, Joseph P.
    Young, Steven D.
    Rowley, Michael
    Lower, Michael W.
    Gottesdiener, Keith M.
    Hazuda, Daria J.
    PHARMACEUTICAL SCIENCE TO IMPROVE THE HUMAN CONDITION: WINNERS AND FINALIST CANDIDATES OF THE PRIX GALIEN USA, INTERNATIONAL, AND PRO BONO HUMANITARIAN AWARDS 2010, 2011, 1222 : 83 - 89
  • [34] OPTIMIZATION OF A POTENT HIV-1 INTEGRASE STRAND TRANSFER INHIBITOR (INSTI): MOLECULAR MODELING, SYNTHESIS AND ANTI-HIV ACTIVITY
    De Grazia, Sara
    Ferro, Stefania
    De Luca, Laura
    Barreca, Maria Letizia
    Debyser, Zeger
    Chimirri, Alba
    DRUGS OF THE FUTURE, 2009, 34 : 140 - 140
  • [35] Development of practical synthetic method for the preparation ofdolutegravir sodium, a potent HIV-1 integrase inhibitor for the treatment of HIV infectious disease
    Yasukata T.
    Aoyama Y.
    Yuki Gosei Kagaku Kyokaishi/Journal of Synthetic Organic Chemistry, 2020, 78 (01): : 2 - 10
  • [36] HIV-1 Integrase Inhibitors That Are Active against Drug-Resistant Integrase Mutants
    Smith, Steven J.
    Zhao, Xue Zhi
    Passos, Dario Oliveira
    Lyumkis, Dmitry
    Burke, Terrence R., Jr.
    Hughes, Stephen H.
    ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, 2020, 64 (09)
  • [37] Pth15: An interfacial inhibitor of HIV-1 integrase that efficiently blocks HIV-1 replication
    Gros, Edwige
    Guiot, Edwire
    Agopian, Audrey
    Deprez, Eric
    Mouscadet, Jean Francois
    Witvrouw, Myriam
    Divita, Gilles
    ANTIVIRAL RESEARCH, 2008, 78 (02) : A28 - A28
  • [38] Binding modes of HIV-1 integrase inhibitors at the active site
    Sotriffer, CA
    Ni, HH
    McCammon, JA
    RATIONAL APPROACHES TO DRUG DESIGN, 2001, : 83 - 87
  • [39] Active site binding modes of HIV-1 integrase inhibitors
    Sotriffer, CA
    Ni, HH
    McCammon, JA
    JOURNAL OF MEDICINAL CHEMISTRY, 2000, 43 (22) : 4109 - 4117
  • [40] Electrochemistry of deferiprone as an orally active iron chelator and HIV-1 replication inhibitor and its determination
    Yadegari, H.
    Jabbari, A.
    Heli, H.
    Moosavi-Movahedi, A. A.
    Majdi, S.
    JOURNAL OF THE BRAZILIAN CHEMICAL SOCIETY, 2008, 19 (05) : 1017 - 1022