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Items: 1 to 20 of 118

1.

Development of potent and selective factor Xa inhibitors.

Rai R, Kolesnikov A, Li Y, Young WB, Leahy E, Sprengeler PA, Verner E, Shrader WD, Burgess-Henry J, Sangalang JC, Allen D, Chen X, Katz BA, Luong C, Elrod K, Cregar L.

Bioorg Med Chem Lett. 2001 Jul 23;11(14):1797-800.

PMID:
11459634
2.

Neutral inhibitors of the serine protease factor Xa.

Shrader WD, Young WB, Sprengeler PA, Sangalang JC, Elrod K, Carr G.

Bioorg Med Chem Lett. 2001 Jul 23;11(14):1801-4.

PMID:
11459635
3.

Exploiting subsite S1 of trypsin-like serine proteases for selectivity: potent and selective inhibitors of urokinase-type plasminogen activator.

Mackman RL, Katz BA, Breitenbucher JG, Hui HC, Verner E, Luong C, Liu L, Sprengeler PA.

J Med Chem. 2001 Nov 8;44(23):3856-71.

PMID:
11689072
4.

Structural basis for selectivity of a small molecule, S1-binding, submicromolar inhibitor of urokinase-type plasminogen activator.

Katz BA, Mackman R, Luong C, Radika K, Martelli A, Sprengeler PA, Wang J, Chan H, Wong L.

Chem Biol. 2000 Apr;7(4):299-312.

5.

2-(2-Hydroxy-3-alkoxyphenyl)-1H-benzimidazole-5-carboxamidine derivatives as potent and selective urokinase-type plasminogen activator inhibitors.

Mackman RL, Hui HC, Breitenbucher JG, Katz BA, Luong C, Martelli A, McGee D, Radika K, Sendzik M, Spencer JR, Sprengeler PA, Tario J, Verner E, Wang J.

Bioorg Med Chem Lett. 2002 Aug 5;12(15):2019-22.

PMID:
12113832
6.

Parallel synthesis and structure-activity relationships of a series of highly potent, selective, and neutral factor Xa inhibitors.

Bauer SM, Goldman EA, Huang W, Su T, Wang L, Woolfrey J, Wu Y, Zuckett JF, Arfsten A, Huang B, Kothule J, Lin J, May B, Sinha U, Wong PW, Hutchaleelaha A, Scarborough RM, Zhu BY.

Bioorg Med Chem Lett. 2004 Aug 2;14(15):4045-50.

PMID:
15225723
7.

Design, structure-activity relationship, and pharmacokinetic profile of pyrazole-based indoline factor Xa inhibitors.

Varnes JG, Wacker DA, Jacobson IC, Quan ML, Ellis CD, Rossi KA, He MY, Luettgen JM, Knabb RM, Bai S, He K, Lam PY, Wexler RR.

Bioorg Med Chem Lett. 2007 Dec 1;17(23):6481-8. Epub 2007 Oct 1.

PMID:
17933529
8.

Design, synthesis, and in vitro biological activity of indole-based factor Xa inhibitors.

Arnaiz DO, Zhao Z, Liang A, Trinh L, Witlow M, Koovakkat SK, Shaw KJ.

Bioorg Med Chem Lett. 2000 May 1;10(9):957-61.

PMID:
10853668
9.

3D-QSAR CoMFA studies on trypsin-like serine protease inhibitors: a comparative selectivity analysis.

Bhongade BA, Gouripur VV, Gadad AK.

Bioorg Med Chem. 2005 Apr 15;13(8):2773-82.

PMID:
15781388
10.

Design, synthesis, and biological evaluation of potent and selective amidino bicyclic factor Xa inhibitors.

Han Q, Dominguez C, Stouten PF, Park JM, Duffy DE, Galemmo RA Jr, Rossi KA, Alexander RS, Smallwood AM, Wong PC, Wright MM, Luettgen JM, Knabb RM, Wexler RR.

J Med Chem. 2000 Nov 16;43(23):4398-415.

PMID:
11087565
11.

Development of serine protease inhibitors displaying a multicentered short (<2.3 A) hydrogen bond binding mode: inhibitors of urokinase-type plasminogen activator and factor Xa.

Verner E, Katz BA, Spencer JR, Allen D, Hataye J, Hruzewicz W, Hui HC, Kolesnikov A, Li Y, Luong C, Martelli A, Radika K, Rai R, She M, Shrader W, Sprengeler PA, Trapp S, Wang J, Young WB, Mackman RL.

J Med Chem. 2001 Aug 16;44(17):2753-71.

PMID:
11495587
12.

Design and quantitative structure-activity relationship of 3-amidinobenzyl-1H-indole-2-carboxamides as potent, nonchiral, and selective inhibitors of blood coagulation factor Xa.

Matter H, Defossa E, Heinelt U, Blohm PM, Schneider D, Müller A, Herok S, Schreuder H, Liesum A, Brachvogel V, Lönze P, Walser A, Al-Obeidi F, Wildgoose P.

J Med Chem. 2002 Jun 20;45(13):2749-69.

PMID:
12061878
14.

Design and synthesis of potent and selective 5,6-fused heterocyclic thrombin inhibitors.

Dominguez C, Duffy DE, Han Q, Alexander RS, Galemmo RA Jr, Park JM, Wong PC, Amparo EC, Knabb RM, Luettgen J, Wexler RR.

Bioorg Med Chem Lett. 1999 Apr 5;9(7):925-30.

PMID:
10230612
15.

Structure- and property-based design of factor Xa inhibitors: pyrrolidin-2-ones with acyclic alanyl amides as P4 motifs.

Young RJ, Campbell M, Borthwick AD, Brown D, Burns-Kurtis CL, Chan C, Convery MA, Crowe MC, Dayal S, Diallo H, Kelly HA, King NP, Kleanthous S, Mason AM, Mordaunt JE, Patel C, Pateman AJ, Senger S, Shah GP, Smith PW, Watson NS, Weston HE, Zhou P.

Bioorg Med Chem Lett. 2006 Dec 1;16(23):5953-7. Epub 2006 Sep 18.

PMID:
16982190
16.

Design and synthesis of orally active pyrrolidin-2-one-based factor Xa inhibitors.

Watson NS, Brown D, Campbell M, Chan C, Chaudry L, Convery MA, Fenwick R, Hamblin JN, Haslam C, Kelly HA, King NP, Kurtis CL, Leach AR, Manchee GR, Mason AM, Mitchell C, Patel C, Patel VK, Senger S, Shah GP, Weston HE, Whitworth C, Young RJ.

Bioorg Med Chem Lett. 2006 Jul 15;16(14):3784-8. Epub 2006 May 11.

PMID:
16697194
17.

Discovery of R-142086 as a factor Xa (FXa) inhibitor: syntheses and structure-activity relationships of cinnamyl derivatives.

Noguchi T, Tanaka N, Nishimata T, Goto R, Hayakawa M, Sugidachi A, Ogawa T, Niitsu Y, Asai F, Ishizuka T, Fujimoto K.

Chem Pharm Bull (Tokyo). 2009 Jan;57(1):22-33.

18.

Design, synthesis, and SAR of substituted acrylamides as factor Xa inhibitors.

Song Y, Clizbe L, Bhakta C, Teng W, Li W, Wu Y, Jia ZJ, Zhang P, Wang L, Doughan B, Su T, Kanter J, Woolfrey J, Wong P, Huang B, Tran K, Sinha U, Park G, Reed A, Malinowski J, Hollenbach S, Scarborough RM, Zhu BY.

Bioorg Med Chem Lett. 2002 Jun 3;12(11):1511-5.

PMID:
12031331
19.

Structure-directed discovery of potent non-peptidic inhibitors of human urokinase that access a novel binding subsite.

Nienaber VL, Davidson D, Edalji R, Giranda VL, Klinghofer V, Henkin J, Magdalinos P, Mantei R, Merrick S, Severin JM, Smith RA, Stewart K, Walter K, Wang J, Wendt M, Weitzberg M, Zhao X, Rockway T.

Structure. 2000 May 15;8(5):553-63.

20.

Preparation of 1-(4-methoxyphenyl)-1H-pyrazolo[4,3-d]pyrimidin-7(6H)-ones as potent, selective and bioavailable inhibitors of coagulation factor Xa.

Fevig JM, Cacciola J, Buriak J Jr, Rossi KA, Knabb RM, Luettgen JM, Wong PC, Bai SA, Wexler RR, Lam PY.

Bioorg Med Chem Lett. 2006 Jul 15;16(14):3755-60. Epub 2006 May 8.

PMID:
16682200
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