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Results: 1 to 20 of 94

1.

P2 pyridine N-oxide thrombin inhibitors: a novel peptidomimetic scaffold.

Nantermet PG, Burgey CS, Robinson KA, Pellicore JM, Newton CL, Deng JZ, Selnick HG, Lewis SD, Lucas BJ, Krueger JA, Miller-Stein C, White RB, Wong B, McMasters DR, Wallace AA, Lynch JJ Jr, Yan Y, Chen Z, Kuo L, Gardell SJ, Shafer JA, Vacca JP, Lyle TA.

Bioorg Med Chem Lett. 2005 Jun 2;15(11):2771-5.

PMID:
15911253
[PubMed - indexed for MEDLINE]
2.

Structure of a novel thrombin inhibitor with an uncharged D-amino acid as P1 residue.

Friedrich R, Riester D, Göttig P, Thürk M, Schwienhorst A, Bode W.

Eur J Med Chem. 2008 Jun;43(6):1330-5. Epub 2007 Sep 9.

PMID:
17950494
[PubMed - indexed for MEDLINE]
3.

Peptidomimetic thrombin inhibitors.

Kikelj D.

Pathophysiol Haemost Thromb. 2003 Sep-2004 Dec;33(5-6):487-91. Review.

PMID:
15692265
[PubMed - indexed for MEDLINE]
4.

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 Jr, Lin JH, Chen IW, Vastag K, Naylor-Olsen AM, Vacca JP.

J Med Chem. 1998 Jan 29;41(3):401-6.

PMID:
9464370
[PubMed - indexed for MEDLINE]
5.

3,4-Dihydro-2H-1,4-benzoxazine derivatives combining thrombin inhibitory and glycoprotein IIb/IIIa receptor antagonistic activity as a novel class of antithrombotic compounds with dual function.

Ilas J, Jakopin Z, Borstnar T, Stegnar M, Kikelj D.

J Med Chem. 2008 Sep 25;51(18):5617-29. doi: 10.1021/jm8003448. Epub 2008 Aug 27.

PMID:
18729445
[PubMed - indexed for MEDLINE]
6.

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 1;18(9):2865-70. doi: 10.1016/j.bmcl.2008.03.087. Epub 2008 Apr 8.

PMID:
18420408
[PubMed - indexed for MEDLINE]
7.

Development of an oxazolopyridine series of dual thrombin/factor Xa inhibitors via structure-guided lead optimization.

Deng JZ, McMasters DR, Rabbat PM, Williams PD, Coburn CA, Yan Y, Kuo LC, Lewis SD, Lucas BJ, Krueger JA, Strulovici B, Vacca JP, Lyle TA, Burgey CS.

Bioorg Med Chem Lett. 2005 Oct 15;15(20):4411-6.

PMID:
16137886
[PubMed - indexed for MEDLINE]
8.

{4(S)-(Piperidin-1-ylcarbonyl)-4-[3-(trifluoromethyl)phenylsulfonamido]butyl}guanidinium chloride: a model of a graftable thrombin inhibitor.

Michaux C, Salvagnini C, Norberg B, Marchand-Brynaert J, Wouters J.

Acta Crystallogr C. 2006 Dec;62(Pt 12):o691-3. Epub 2006 Nov 22.

PMID:
17148914
[PubMed - indexed for MEDLINE]
9.

Discovery of potent, selective 4-fluoroproline-based thrombin inhibitors with improved metabolic stability.

Staas DD, Savage KL, Sherman VL, Shimp HL, Lyle TA, Tran LO, Wiscount CM, McMasters DR, Sanderson PE, Williams PD, Lucas BJ Jr, Krueger JA, Lewis SD, White RB, Yu S, Wong BK, Kochansky CJ, Anari MR, Yan Y, Vacca JP.

Bioorg Med Chem. 2006 Oct 15;14(20):6900-16. Epub 2006 Jul 25.

PMID:
16870455
[PubMed - indexed for MEDLINE]
10.

Phenolic P2/P3 core motif as thrombin inhibitors--design, synthesis, and X-ray co-crystal structure.

Hanessian S, Therrien E, van Otterlo WA, Bayrakdarian M, Nilsson I, Fjellström O, Xue Y.

Bioorg Med Chem Lett. 2006 Feb 15;16(4):1032-6. Epub 2005 Nov 15.

PMID:
16290930
[PubMed - indexed for MEDLINE]
11.
12.

Novel pyrazinone and pyridinone thrombin inhibitors incorporating weakly basic heterobicyclic P(1)-arginine mimetics.

Kranjc A, Masic LP, Reven S, Mikic K, Prezelj A, Stegnar M, Kikelj D.

Eur J Med Chem. 2005 Aug;40(8):782-91.

PMID:
15890436
[PubMed - indexed for MEDLINE]
13.

In vitro evaluation and crystallographic analysis of a new class of selective, non-amide-based thrombin inhibitors.

Lu T, Tomczuk B, Illig CR, Bone R, Murphy L, Spurlino J, Salemme FR, Soll RM.

Bioorg Med Chem Lett. 1998 Jul 7;8(13):1595-600. Erratum in: Bioorg Med Chem Lett 1998 Sep 22;8(18):2621.

PMID:
9873397
[PubMed - indexed for MEDLINE]
14.

Novel bicyclic lactam inhibitors of thrombin: potency and selectivity optimization through P1 residues.

Lévesque S, St-Denis Y, Bachand B, Préville P, Leblond L, Winocour PD, Edmunds JJ, Rubin JR, Siddiqui MA.

Bioorg Med Chem Lett. 2001 Dec 17;11(24):3161-4.

PMID:
11720865
[PubMed - indexed for MEDLINE]
15.

The design of potent and selective inhibitors of thrombin utilizing a piperazinedione template: part 1.

Cody WL, Cai C, Doherty AM, Edmunds JJ, He JX, Narasimhan LS, Plummer JS, Rapundalo ST, Rubin JR, Van Huis CA, St-Denis Y, Winocour PD, Siddiqui MA.

Bioorg Med Chem Lett. 1999 Sep 6;9(17):2497-502.

PMID:
10498196
[PubMed - indexed for MEDLINE]
16.

Scaffold oriented synthesis. Part 2: Design, synthesis and biological evaluation of pyrimido-diazepines as receptor tyrosine kinase inhibitors.

Gracias V, Ji Z, Akritopoulou-Zanze I, Abad-Zapatero C, Huth JR, Song D, Hajduk PJ, Johnson EF, Glaser KB, Marcotte PA, Pease L, Soni NB, Stewart KD, Davidsen SK, Michaelides MR, Djuric SW.

Bioorg Med Chem Lett. 2008 Apr 15;18(8):2691-5. doi: 10.1016/j.bmcl.2008.03.021. Epub 2008 Mar 10.

PMID:
18362070
[PubMed - indexed for MEDLINE]
17.

Entry into a new class of protein kinase inhibitors by pseudo ring design.

Furet P, Caravatti G, Guagnano V, Lang M, Meyer T, Schoepfer J.

Bioorg Med Chem Lett. 2008 Feb 1;18(3):897-900. doi: 10.1016/j.bmcl.2007.12.041. Epub 2008 Jan 14.

PMID:
18248988
[PubMed - indexed for MEDLINE]
18.

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. Epub 2006 Mar 6.

PMID:
16517159
[PubMed - indexed for MEDLINE]
19.

Bis[2,4-diamino-5-(3,4,5-trimethoxybenzyl)pyrimidin-1-ium] DL-malate.

Franklin S, Balasubramanian T, Varghese B.

Acta Crystallogr C. 2009 Feb;65(Pt 2):o62-5. doi: 10.1107/S0108270109000237. Epub 2009 Jan 14.

PMID:
19190390
[PubMed - indexed for MEDLINE]
20.

Design, synthesis and biological evaluation of thrombin inhibitors based on a pyridine scaffold.

Blomberg D, Fex T, Xue Y, Brickmann K, Kihlberg J.

Org Biomol Chem. 2007 Aug 21;5(16):2599-605.

PMID:
18019535
[PubMed - indexed for MEDLINE]
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