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Journal Abstract Search

254 related items for PubMed ID: 16821774

  • 1. Design, synthesis, and biological evaluation of the combinatorial library with a new spirodiketopiperazine scaffold. Discovery of novel potent and selective low-molecular-weight CCR5 antagonists.
    Habashita H, Kokubo M, Hamano S, Hamanaka N, Toda M, Shibayama S, Tada H, Sagawa K, Fukushima D, Maeda K, Mitsuya H.
    J Med Chem; 2006 Jul 13; 49(14):4140-52. PubMed ID: 16821774
    [Abstract] [Full Text] [Related]

  • 2. Spirodiketopiperazine-based CCR5 inhibitor which preserves CC-chemokine/CCR5 interactions and exerts potent activity against R5 human immunodeficiency virus type 1 in vitro.
    Maeda K, Nakata H, Koh Y, Miyakawa T, Ogata H, Takaoka Y, Shibayama S, Sagawa K, Fukushima D, Moravek J, Koyanagi Y, Mitsuya H.
    J Virol; 2004 Aug 13; 78(16):8654-62. PubMed ID: 15280474
    [Abstract] [Full Text] [Related]

  • 3. Spirodiketopiperazine-based CCR5 antagonists: Lead optimization from biologically active metabolite.
    Nishizawa R, Nishiyama T, Hisaichi K, Matsunaga N, Minamoto C, Habashita H, Takaoka Y, Toda M, Shibayama S, Tada H, Sagawa K, Fukushima D, Maeda K, Mitsuya H.
    Bioorg Med Chem Lett; 2007 Feb 01; 17(3):727-31. PubMed ID: 17118654
    [Abstract] [Full Text] [Related]

  • 4. CCR5 antagonists as anti-HIV-1 agents. Part 3: Synthesis and biological evaluation of piperidine-4-carboxamide derivatives.
    Imamura S, Nishikawa Y, Ichikawa T, Hattori T, Matsushita Y, Hashiguchi S, Kanzaki N, Iizawa Y, Baba M, Sugihara Y.
    Bioorg Med Chem; 2005 Jan 17; 13(2):397-416. PubMed ID: 15598561
    [Abstract] [Full Text] [Related]

  • 5. Novel low molecular weight spirodiketopiperazine derivatives potently inhibit R5 HIV-1 infection through their antagonistic effects on CCR5.
    Maeda K, Yoshimura K, Shibayama S, Habashita H, Tada H, Sagawa K, Miyakawa T, Aoki M, Fukushima D, Mitsuya H.
    J Biol Chem; 2001 Sep 14; 276(37):35194-200. PubMed ID: 11454872
    [Abstract] [Full Text] [Related]

  • 6. TAK-652 inhibits CCR5-mediated human immunodeficiency virus type 1 infection in vitro and has favorable pharmacokinetics in humans.
    Baba M, Takashima K, Miyake H, Kanzaki N, Teshima K, Wang X, Shiraishi M, Iizawa Y.
    Antimicrob Agents Chemother; 2005 Nov 14; 49(11):4584-91. PubMed ID: 16251299
    [Abstract] [Full Text] [Related]

  • 7. Molecular interactions of CCR5 with major classes of small-molecule anti-HIV CCR5 antagonists.
    Kondru R, Zhang J, Ji C, Mirzadegan T, Rotstein D, Sankuratri S, Dioszegi M.
    Mol Pharmacol; 2008 Mar 14; 73(3):789-800. PubMed ID: 18096812
    [Abstract] [Full Text] [Related]

  • 8. Orally active CCR5 antagonists as anti-HIV-1 agents. Part 3: Synthesis and biological activities of 1-benzazepine derivatives containing a sulfoxide moiety.
    Seto M, Miyamoto N, Aikawa K, Aramaki Y, Kanzaki N, Iizawa Y, Baba M, Shiraishi M.
    Bioorg Med Chem; 2005 Jan 17; 13(2):363-86. PubMed ID: 15598559
    [Abstract] [Full Text] [Related]

  • 9. Potent anti-R5 human immunodeficiency virus type 1 effects of a CCR5 antagonist, AK602/ONO4128/GW873140, in a novel human peripheral blood mononuclear cell nonobese diabetic-SCID, interleukin-2 receptor gamma-chain-knocked-out AIDS mouse model.
    Nakata H, Maeda K, Miyakawa T, Shibayama S, Matsuo M, Takaoka Y, Ito M, Koyanagi Y, Mitsuya H.
    J Virol; 2005 Feb 17; 79(4):2087-96. PubMed ID: 15681411
    [Abstract] [Full Text] [Related]

  • 10. Highly potent and orally active CCR5 antagonists as anti-HIV-1 agents: synthesis and biological activities of 1-benzazocine derivatives containing a sulfoxide moiety.
    Seto M, Aikawa K, Miyamoto N, Aramaki Y, Kanzaki N, Takashima K, Kuze Y, Iizawa Y, Baba M, Shiraishi M.
    J Med Chem; 2006 Mar 23; 49(6):2037-48. PubMed ID: 16539392
    [Abstract] [Full Text] [Related]

  • 11. [2-(4-Phenyl-4-piperidinyl)ethyl]amine based CCR5 antagonists: derivatizations at the N-terminal of the piperidine ring.
    Duan M, Aquino C, Ferris R, Kazmierski WM, Kenakin T, Koble C, Wheelan P, Watson C, Youngman M.
    Bioorg Med Chem Lett; 2009 Mar 15; 19(6):1610-3. PubMed ID: 19233649
    [Abstract] [Full Text] [Related]

  • 12. Design, synthesis, and biological evaluation of novel 2-methylpiperazine derivatives as potent CCR5 antagonists.
    Hu S, Wang Z, Hou T, Ma X, Li J, Liu T, Xie X, Hu Y.
    Bioorg Med Chem; 2015 Mar 01; 23(5):1157-68. PubMed ID: 25638498
    [Abstract] [Full Text] [Related]

  • 13. Identification and characterization of INCB9471, an allosteric noncompetitive small-molecule antagonist of C-C chemokine receptor 5 with potent inhibitory activity against monocyte migration and HIV-1 infection.
    Shin N, Solomon K, Zhou N, Wang KH, Garlapati V, Thomas B, Li Y, Covington M, Baribaud F, Erickson-Viitanen S, Czerniak P, Contel N, Liu P, Burn T, Hollis G, Yeleswaram S, Vaddi K, Xue CB, Metcalf B, Friedman S, Scherle P, Newton R.
    J Pharmacol Exp Ther; 2011 Jul 01; 338(1):228-39. PubMed ID: 21459966
    [Abstract] [Full Text] [Related]

  • 14. CCR5 antagonists as anti-HIV-1 agents. Part 2: Synthesis and biological evaluation of N-[3-(4-benzylpiperidin-1-yl)propyl]-N,N'-diphenylureas.
    Imamura S, Kurasawa O, Nara Y, Ichikawa T, Nishikawa Y, Iida T, Hashiguchi S, Kanzaki N, Iizawa Y, Baba M, Sugihara Y.
    Bioorg Med Chem; 2004 May 01; 12(9):2295-306. PubMed ID: 15080927
    [Abstract] [Full Text] [Related]

  • 15. Generation of predictive pharmacophore models for CCR5 antagonists: study with piperidine- and piperazine-based compounds as a new class of HIV-1 entry inhibitors.
    Debnath AK.
    J Med Chem; 2003 Oct 09; 46(21):4501-15. PubMed ID: 14521412
    [Abstract] [Full Text] [Related]

  • 16. [CCR5, a new target of anti-HIV drugs].
    Han YX, Jiang JD.
    Zhongguo Yi Xue Ke Xue Yuan Xue Bao; 2003 Oct 09; 25(5):635-9. PubMed ID: 14650176
    [Abstract] [Full Text] [Related]

  • 17. 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.
    Tagat JR, McCombie SW, Nazareno D, Labroli MA, Xiao Y, Steensma RW, Strizki JM, Baroudy BM, Cox K, Lachowicz J, Varty G, Watkins R.
    J Med Chem; 2004 May 06; 47(10):2405-8. PubMed ID: 15115380
    [Abstract] [Full Text] [Related]

  • 18. Discovery of novel (S)-alpha-phenyl-gamma-amino butanamide containing CCR5 antagonists via functionality inversion approach.
    Zhang HS, Feng DZ, Chen L, Long YQ.
    Bioorg Med Chem Lett; 2010 Apr 01; 20(7):2219-23. PubMed ID: 20207141
    [Abstract] [Full Text] [Related]

  • 19. Discovery of N-benzyl-N'-(4-pipyridinyl)urea CCR5 antagonists as anti-HIV-1 agents (II): modification of the acyl portion.
    Duan M, Peckham J, Edelstein M, Ferris R, Kazmierski WM, Spaltenstein A, Wheelan P, Xiong Z.
    Bioorg Med Chem Lett; 2010 Dec 15; 20(24):7401-4. PubMed ID: 21055933
    [Abstract] [Full Text] [Related]

  • 20. Peptide, peptidomimetic and small-molecule drug discovery targeting HIV-1 host-cell attachment and entry through gp120, gp41, CCR5 and CXCR4.
    Kazmierski WM, Kenakin TP, Gudmundsson KS.
    Chem Biol Drug Des; 2006 Jan 15; 67(1):13-26. PubMed ID: 16492145
    [Abstract] [Full Text] [Related]

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