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Journal Abstract Search

115 related items for PubMed ID: 9464370

  • 1. Discovery and development of the novel potent orally active thrombin inhibitor N-(9-hydroxy-9-fluorenecarboxy)prolyl trans-4-aminocyclohexylmethyl amide (L-372,460): coapplication of structure-based design and rapid multiple analogue synthesis on solid support.
    Brady SF, Stauffer KJ, Lumma WC, Smith GM, Ramjit HG, Lewis SD, Lucas BJ, Gardell SJ, Lyle EA, Appleby SD, Cook JJ, Holahan MA, Stranieri MT, Lynch JJ, Lin JH, Chen IW, Vastag K, Naylor-Olsen AM, Vacca JP.
    J Med Chem; 1998 Jan 29; 41(3):401-6. PubMed ID: 9464370
    [Abstract] [Full Text] [Related]

  • 2. Efficacious and orally bioavailable thrombin inhibitors based on a 2,5-thienylamidine at the P1 position: discovery of N-carboxymethyl-d-diphenylalanyl-l-prolyl[(5-amidino-2-thienyl)methyl]amide.
    Lee K, Park CW, Jung WH, Park HD, Lee SH, Chung KH, Park SK, Kwon OH, Kang M, Park DH, Lee SK, Kim EE, Yoon SK, Kim A.
    J Med Chem; 2003 Aug 14; 46(17):3612-22. PubMed ID: 12904065
    [Abstract] [Full Text] [Related]

  • 3. 9-hydroxyazafluorenes and their use in thrombin inhibitors.
    Stauffer KJ, Williams PD, Selnick HG, Nantermet PG, Newton CL, Homnick CF, Zrada MM, Lewis SD, Lucas BJ, Krueger JA, Pietrak BL, Lyle EA, Singh R, Miller-Stein C, White RB, Wong B, Wallace AA, Sitko GR, Cook JJ, Holahan MA, Stranieri-Michener M, Leonard YM, Lynch JJ, McMasters DR, Yan Y.
    J Med Chem; 2005 Apr 07; 48(7):2282-93. PubMed ID: 15801822
    [Abstract] [Full Text] [Related]

  • 4. Structure-based design of novel groups for use in the P1 position of thrombin inhibitor scaffolds. Part 2: N-acetamidoimidazoles.
    Isaacs RC, Solinsky MG, Cutrona KJ, Newton CL, Naylor-Olsen AM, McMasters DR, Krueger JA, Lewis SD, Lucas BJ, Kuo LC, Yan Y, Lynch JJ, Lyle EA.
    Bioorg Med Chem Lett; 2008 Mar 15; 18(6):2062-6. PubMed ID: 18291642
    [Abstract] [Full Text] [Related]

  • 5. Discovery of a novel, selective, and orally bioavailable class of thrombin inhibitors incorporating aminopyridyl moieties at the P1 position.
    Feng DM, Gardell SJ, Lewis SD, Bock MG, Chen Z, Freidinger RM, Naylor-Olsen AM, Ramjit HG, Woltmann R, Baskin EP, Lynch JJ, Lucas R, Shafer JA, Dancheck KB, Chen IW, Mao SS, Krueger JA, Hare TR, Mulichak AM, Vacca JP.
    J Med Chem; 1997 Nov 07; 40(23):3726-33. PubMed ID: 9371237
    [Abstract] [Full Text] [Related]

  • 6. Discovery of trans-4-[1-[[2,5-Dichloro-4-(1-methyl-3-indolylcarboxamido)phenyl]acetyl]-(4S)-methoxy-(2S)-pyrrolidinylmethoxy]cyclohexanecarboxylic acid: an orally active, selective very late antigen-4 antagonist.
    Muro F, Iimura S, Sugimoto Y, Yoneda Y, Chiba J, Watanabe T, Setoguchi M, Iigou Y, Matsumoto K, Satoh A, Takayama G, Taira T, Yokoyama M, Takashi T, Nakayama A, Machinaga N.
    J Med Chem; 2009 Dec 24; 52(24):7974-92. PubMed ID: 19891440
    [Abstract] [Full Text] [Related]

  • 7. Orally active thrombin inhibitors. Part 1: optimization of the P1-moiety.
    Mack H, Baucke D, Hornberger W, Lange UE, Seitz W, Höffken HW.
    Bioorg Med Chem Lett; 2006 May 15; 16(10):2641-7. PubMed ID: 16517159
    [Abstract] [Full Text] [Related]

  • 8. Design, synthesis, and evolution of a novel, selective, and orally bioavailable class of thrombin inhibitors: P1-argininal derivatives incorporating P3-P4 lactam sulfonamide moieties.
    Semple JE, Rowley DC, Brunck TK, Ha-Uong T, Minami NK, Owens TD, Tamura SY, Goldman EA, Siev DV, Ardecky RJ, Carpenter SH, Ge Y, Richard BM, Nolan TG, Håkanson K, Tulinsky A, Nutt RF, Ripka WC.
    J Med Chem; 1996 Nov 08; 39(23):4531-6. PubMed ID: 8917639
    [No Abstract] [Full Text] [Related]

  • 9. Orally active thrombin inhibitors. Part 2: optimization of the P2-moiety.
    Lange UE, Baucke D, Hornberger W, Mack H, Seitz W, Höffken HW.
    Bioorg Med Chem Lett; 2006 May 15; 16(10):2648-53. PubMed ID: 16460939
    [Abstract] [Full Text] [Related]

  • 10. Discovery of novel 2,8-diazaspiro[4.5]decanes as orally active glycoprotein IIb-IIIa antagonists.
    Mehrotra MM, Heath JA, Smyth MS, Pandey A, Rose JW, Seroogy JM, Volkots DL, Nannizzi-Alaimo L, Park GL, Lambing JL, Hollenbach SJ, Scarborough RM.
    J Med Chem; 2004 Apr 08; 47(8):2037-61. PubMed ID: 15056002
    [Abstract] [Full Text] [Related]

  • 11. Design and synthesis of a series of potent and orally bioavailable noncovalent thrombin inhibitors that utilize nonbasic groups in the P1 position.
    Tucker TJ, Brady SF, Lumma WC, Lewis SD, Gardell SJ, Naylor-Olsen AM, Yan Y, Sisko JT, Stauffer KJ, Lucas BJ, Lynch JJ, Cook JJ, Stranieri MT, Holahan MA, Lyle EA, Baskin EP, Chen IW, Dancheck KB, Krueger JA, Cooper CM, Vacca JP.
    J Med Chem; 1998 Aug 13; 41(17):3210-9. PubMed ID: 9703466
    [Abstract] [Full Text] [Related]

  • 12. Design of novel, potent, noncovalent inhibitors of thrombin with nonbasic P-1 substructures: rapid structure-activity studies by solid-phase synthesis.
    Lumma WC, Witherup KM, Tucker TJ, Brady SF, Sisko JT, Naylor-Olsen AM, Lewis SD, Lucas BJ, Vacca JP.
    J Med Chem; 1998 Mar 26; 41(7):1011-3. PubMed ID: 9544200
    [Abstract] [Full Text] [Related]

  • 13. In-depth study of tripeptide-based alpha-ketoheterocycles as inhibitors of thrombin. Effective utilization of the S1' subsite and its implications to structure-based drug design.
    Costanzo MJ, Almond HR, Hecker LR, Schott MR, Yabut SC, Zhang HC, Andrade-Gordon P, Corcoran TW, Giardino EC, Kauffman JA, Lewis JM, de Garavilla L, Haertlein BJ, Maryanoff BE.
    J Med Chem; 2005 Mar 24; 48(6):1984-2008. PubMed ID: 15771442
    [Abstract] [Full Text] [Related]

  • 14. Metabolism-directed optimization of 3-aminopyrazinone acetamide thrombin inhibitors. Development of an orally bioavailable series containing P1 and P3 pyridines.
    Burgey CS, Robinson KA, Lyle TA, Sanderson PE, Lewis SD, Lucas BJ, Krueger JA, Singh R, Miller-Stein C, White RB, Wong B, Lyle EA, Williams PD, Coburn CA, Dorsey BD, Barrow JC, Stranieri MT, Holahan MA, Sitko GR, Cook JJ, McMasters DR, McDonough CM, Sanders WM, Wallace AA, Clayton FC, Bohn D, Leonard YM, Detwiler TJ, Lynch JJ, Yan Y, Chen Z, Kuo L, Gardell SJ, Shafer JA, Vacca JP.
    J Med Chem; 2003 Feb 13; 46(4):461-73. PubMed ID: 12570369
    [Abstract] [Full Text] [Related]

  • 15. Dicarboxylic acid azacycle l-prolyl-pyrrolidine amides as prolyl oligopeptidase inhibitors and three-dimensional quantitative structure-activity relationship of the enzyme-inhibitor interactions.
    Jarho EM, Wallén EA, Christiaans JA, Forsberg MM, Venäläinen JI, Männistö PT, Gynther J, Poso A.
    J Med Chem; 2005 Jul 28; 48(15):4772-82. PubMed ID: 16033257
    [Abstract] [Full Text] [Related]

  • 16. Synthesis of a series of potent and orally bioavailable thrombin inhibitors that utilize 3,3-disubstituted propionic acid derivatives in the P3 position.
    Tucker TJ, Lumma WC, Lewis SD, Gardell SJ, Lucas BJ, Sisko JT, Lynch JJ, Lyle EA, Baskin EP, Woltmann RF, Appleby SD, Chen IW, Dancheck KB, Naylor-Olsen AM, Krueger JA, Cooper CM, Vacca JP.
    J Med Chem; 1997 Oct 24; 40(22):3687-93. PubMed ID: 9357536
    [Abstract] [Full Text] [Related]

  • 17. Structure-based design and synthesis of non-nucleoside, potent, and orally bioavailable adenosine deaminase inhibitors.
    Terasaka T, Okumura H, Tsuji K, Kato T, Nakanishi I, Kinoshita T, Kato Y, Kuno M, Seki N, Naoe Y, Inoue T, Tanaka K, Nakamura K.
    J Med Chem; 2004 May 20; 47(11):2728-31. PubMed ID: 15139750
    [Abstract] [Full Text] [Related]

  • 18. Orally efficacious thrombin inhibitors with cyanofluorophenylacetamide as the P2 motif.
    Kreutter KD, Lu T, Lee L, Giardino EC, Patel S, Huang H, Xu G, Fitzgerald M, Haertlein BJ, Mohan V, Crysler C, Eisennagel S, Dasgupta M, McMillan M, Spurlino JC, Huebert ND, Maryanoff BE, Tomczuk BE, Damiano BP, Player MR.
    Bioorg Med Chem Lett; 2008 May 01; 18(9):2865-70. PubMed ID: 18420408
    [Abstract] [Full Text] [Related]

  • 19. Design, synthesis, and SAR of anthranilamide-based factor Xa inhibitors with improved functional activity.
    Zhang P, Bao L, Zuckett JF, Jia ZJ, Woolfrey J, Arfsten A, Edwards S, Sinha U, Hutchaleelaha A, Lambing JL, Hollenbach SJ, Scarborough RM, Zhu BY.
    Bioorg Med Chem Lett; 2004 Feb 23; 14(4):989-93. PubMed ID: 15013007
    [Abstract] [Full Text] [Related]

  • 20. Oxyguanidines. Part 2: Discovery of a novel orally active thrombin inhibitor through structure-based drug design and parallel synthesis.
    Lu T, Markotan T, Coppo F, Tomczuk B, Crysler C, Eisennagel S, Spurlino J, Gremminger L, Soll RM, Giardino EC, Bone R.
    Bioorg Med Chem Lett; 2004 Jul 16; 14(14):3727-31. PubMed ID: 15203151
    [Abstract] [Full Text] [Related]

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