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Journal Abstract Search

232 related items for PubMed ID: 14521405

  • 1. Structure-based design of novel guanidine/benzamidine mimics: potent and orally bioavailable factor Xa inhibitors as novel anticoagulants.
    Lam PY, Clark CG, Li R, Pinto DJ, Orwat MJ, Galemmo RA, Fevig JM, Teleha CA, Alexander RS, Smallwood AM, Rossi KA, Wright MR, Bai SA, He K, Luettgen JM, Wong PC, Knabb RM, Wexler RR.
    J Med Chem; 2003 Oct 09; 46(21):4405-18. PubMed ID: 14521405
    [Abstract] [Full Text] [Related]

  • 2. Anthranilamide-based N,N-dialkylbenzamidines as potent and orally bioavailable factor Xa inhibitors: P4 SAR.
    Zhang P, Bao L, Fan J, Jia ZJ, Sinha U, Wong PW, Park G, Hutchaleelaha A, Scarborough RM, Zhu BY.
    Bioorg Med Chem Lett; 2009 Apr 15; 19(8):2186-9. PubMed ID: 19297158
    [Abstract] [Full Text] [Related]

  • 3. 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]

  • 4. Discovery of an orally efficacious inhibitor of coagulation factor Xa which incorporates a neutral P1 ligand.
    Choi-Sledeski YM, Kearney R, Poli G, Pauls H, Gardner C, Gong Y, Becker M, Davis R, Spada A, Liang G, Chu V, Brown K, Collussi D, Leadley R, Rebello S, Moxey P, Morgan S, Bentley R, Kasiewski C, Maignan S, Guilloteau JP, Mikol V.
    J Med Chem; 2003 Feb 27; 46(5):681-4. PubMed ID: 12593648
    [Abstract] [Full Text] [Related]

  • 5. 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]

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  • 7. Exploration of potential prodrugs of RWJ-445167, an oxyguanidine-based dual inhibitor of thrombin and factor Xa.
    Maryanoff BE, McComsey DF, Costanzo MJ, Yabut SC, Lu T, Player MR, Giardino EC, Damiano BP.
    Chem Biol Drug Des; 2006 Jul 24; 68(1):29-36. PubMed ID: 16923023
    [Abstract] [Full Text] [Related]

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  • 9. Discovery of 1-(3'-aminobenzisoxazol-5'-yl)-3-trifluoromethyl-N-[2-fluoro-4- [(2'-dimethylaminomethyl)imidazol-1-yl]phenyl]-1H-pyrazole-5-carboxyamide hydrochloride (razaxaban), a highly potent, selective, and orally bioavailable factor Xa inhibitor.
    Quan ML, Lam PY, Han Q, Pinto DJ, He MY, Li R, Ellis CD, Clark CG, Teleha CA, Sun JH, Alexander RS, Bai S, Luettgen JM, Knabb RM, Wong PC, Wexler RR.
    J Med Chem; 2005 Mar 24; 48(6):1729-44. PubMed ID: 15771420
    [Abstract] [Full Text] [Related]

  • 10. Sulfonamidolactam inhibitors of coagulation factor Xa.
    Smallheer JM, Wang S, Laws ML, Nakajima S, Hu Z, Han W, Jacobson I, Luettgen JM, Rossi KA, Rendina AR, Knabb RM, Wexler RR, Lam PY, Quan ML.
    Bioorg Med Chem Lett; 2008 Apr 01; 18(7):2428-33. PubMed ID: 18329876
    [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. 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]

  • 13. Rational design, synthesis, and structure-activity relationships of novel factor Xa inhibitors: (2-substituted-4-amidinophenyl)pyruvic and -propionic acids.
    Sagi K, Nakagawa T, Yamanashi M, Makino S, Takahashi M, Takayanagi M, Takenaka K, Suzuki N, Oono S, Kataoka N, Ishikawa K, Shima S, Fukuda Y, Kayahara T, Takehana S, Shima Y, Tashiro K, Yamamoto H, Yoshimoto R, Iwata S, Tsuji T, Sakurai K, Shoji M.
    J Med Chem; 2003 May 08; 46(10):1845-57. PubMed ID: 12723948
    [Abstract] [Full Text] [Related]

  • 14. 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]

  • 15. Discovery of the novel antithrombotic agent 5-chloro-N-({(5S)-2-oxo-3- [4-(3-oxomorpholin-4-yl)phenyl]-1,3-oxazolidin-5-yl}methyl)thiophene- 2-carboxamide (BAY 59-7939): an oral, direct factor Xa inhibitor.
    Roehrig S, Straub A, Pohlmann J, Lampe T, Pernerstorfer J, Schlemmer KH, Reinemer P, Perzborn E.
    J Med Chem; 2005 Sep 22; 48(19):5900-8. PubMed ID: 16161994
    [Abstract] [Full Text] [Related]

  • 16. Discovery of 1-(4-methoxyphenyl)-7-oxo-6-(4-(2-oxopiperidin-1-yl)phenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide (apixaban, BMS-562247), a highly potent, selective, efficacious, and orally bioavailable inhibitor of blood coagulation factor Xa.
    Pinto DJ, Orwat MJ, Koch S, Rossi KA, Alexander RS, Smallwood A, Wong PC, Rendina AR, Luettgen JM, Knabb RM, He K, Xin B, Wexler RR, Lam PY.
    J Med Chem; 2007 Nov 01; 50(22):5339-56. PubMed ID: 17914785
    [Abstract] [Full Text] [Related]

  • 17. Orally active factor Xa inhibitors: investigation of a novel series of 3-amidinophenylsulfonamide derivatives using an amidoxime prodrug strategy.
    Uchida M, Okazaki K, Mukaiyama H, Isawa H, Kobayashi H, Shiohara H, Muranaka H, Kai Y, Kikuchi N, Takeuchi H, Yokoyama K, Tsuji E, Ozawa T, Hoyano Y, Koizumi T, Misawa K, Hara K, Nakano S, Murakami Y, Okuno H.
    Bioorg Med Chem Lett; 2008 Aug 15; 18(16):4682-7. PubMed ID: 18667303
    [Abstract] [Full Text] [Related]

  • 18. Design of benzamidine-type inhibitors of factor Xa.
    Gabriel B, Stubbs MT, Bergner A, Hauptmann J, Bode W, Stürzebecher J, Moroder L.
    J Med Chem; 1998 Oct 22; 41(22):4240-50. PubMed ID: 9784099
    [Abstract] [Full Text] [Related]

  • 19. Probing the subpockets of factor Xa reveals two binding modes for inhibitors based on a 2-carboxyindole scaffold: a study combining structure-activity relationship and X-ray crystallography.
    Nazaré M, Will DW, Matter H, Schreuder H, Ritter K, Urmann M, Essrich M, Bauer A, Wagner M, Czech J, Lorenz M, Laux V, Wehner V.
    J Med Chem; 2005 Jul 14; 48(14):4511-25. PubMed ID: 15999990
    [Abstract] [Full Text] [Related]

  • 20. Discovery of 1-(2-aminomethylphenyl)-3-trifluoromethyl-N- [3-fluoro-2'-(aminosulfonyl)[1,1'-biphenyl)]-4-yl]-1H-pyrazole-5-carboxyamide (DPC602), a potent, selective, and orally bioavailable factor Xa inhibitor(1).
    Pruitt JR, Pinto DJ, Galemmo RA, Alexander RS, Rossi KA, Wells BL, Drummond S, Bostrom LL, Burdick D, Bruckner R, Chen H, Smallwood A, Wong PC, Wright MR, Bai S, Luettgen JM, Knabb RM, Lam PY, Wexler RR.
    J Med Chem; 2003 Dec 04; 46(25):5298-315. PubMed ID: 14640539
    [Abstract] [Full Text] [Related]

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