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Items: 1 to 20 of 439

1.

Potent triazolyl-proline-based inhibitors of HCV NS3 protease.

Naud J, Lemke C, Goudreau N, Beaulieu E, White PD, Llinàs-Brunet M, Forgione P.

Bioorg Med Chem Lett. 2008 Jun 1;18(11):3400-4. doi: 10.1016/j.bmcl.2008.04.012. Epub 2008 Apr 10.

PMID:
18448339
2.

Discovery of novel, potent and bioavailable proline-urea based macrocyclic HCV NS3/4A protease inhibitors.

Vendeville S, Nilsson M, de Kock H, Lin TI, Antonov D, Classon B, Ayesa S, Ivanov V, Johansson PO, Kahnberg P, Eneroth A, Wikstrom K, Vrang L, Edlund M, Lindström S, Van de Vreken W, McGowan D, Tahri A, Hu L, Lenz O, Delouvroy F, Van Dooren M, Kindermans N, Surleraux D, Wigerinck P, Rosenquist A, Samuelsson B, Simmen K, Raboisson P.

Bioorg Med Chem Lett. 2008 Dec 1;18(23):6189-93. doi: 10.1016/j.bmcl.2008.10.004. Epub 2008 Oct 5.

PMID:
18954982
3.

Key steps in the structure-based optimization of the hepatitis C virus NS3/4A protease inhibitor SCH503034.

Madison V, Prongay AJ, Guo Z, Yao N, Pichardo J, Fischmann T, Strickland C, Myers J Jr, Weber PC, Beyer BM, Ingram R, Hong Z, Prosise WW, Ramanathan L, Taremi SS, Yarosh-Tomaine T, Zhang R, Senior M, Yang RS, Malcolm B, Arasappan A, Bennett F, Bogen SL, Chen K, Jao E, Liu YT, Lovey RG, Saksena AK, Venkatraman S, Girijavallabhan V, Njoroge FG.

J Synchrotron Radiat. 2008 May;15(Pt 3):204-7. doi: 10.1107/S0909049507064229. Epub 2008 Apr 18.

4.

Synthesis and optimization of a novel series of HCV NS3 protease inhibitors: 4-arylproline analogs.

Bilodeau F, Bailey MD, Bhardwaj PK, Bordeleau J, Forgione P, Garneau M, Ghiro E, Gorys V, Halmos T, Jolicoeur ES, Leblanc M, Lemke CT, Naud J, O'Meara J, White PW, Llinàs-Brunet M.

Bioorg Med Chem Lett. 2013 Jul 15;23(14):4267-71. doi: 10.1016/j.bmcl.2013.03.043. Epub 2013 Mar 19.

PMID:
23735741
5.

Structure-activity study on a novel series of macrocyclic inhibitors of the hepatitis C virus NS3 protease leading to the discovery of BILN 2061.

Llinàs-Brunet M, Bailey MD, Bolger G, Brochu C, Faucher AM, Ferland JM, Garneau M, Ghiro E, Gorys V, Grand-Maître C, Halmos T, Lapeyre-Paquette N, Liard F, Poirier M, Rhéaume M, Tsantrizos YS, Lamarre D.

J Med Chem. 2004 Mar 25;47(7):1605-8.

PMID:
15027850
6.

Challenges in modern drug discovery: a case study of boceprevir, an HCV protease inhibitor for the treatment of hepatitis C virus infection.

Njoroge FG, Chen KX, Shih NY, Piwinski JJ.

Acc Chem Res. 2008 Jan;41(1):50-9. doi: 10.1021/ar700109k. Review.

PMID:
18193821
7.

Inhibitors of hepatitis C virus NS3.4A protease. Part 3: P2 proline variants.

Perni RB, Farmer LJ, Cottrell KM, Court JJ, Courtney LF, Deininger DD, Gates CA, Harbeson SL, Kim JL, Lin C, Lin K, Luong YP, Maxwell JP, Murcko MA, Pitlik J, Rao BG, Schairer WC, Tung RD, Van Drie JH, Wilson K, Thomson JA.

Bioorg Med Chem Lett. 2004 Apr 19;14(8):1939-42.

PMID:
15050632
8.

Synthesis of new acylsulfamoyl benzoxaboroles as potent inhibitors of HCV NS3 protease.

Li X, Zhang YK, Liu Y, Zhang S, Ding CZ, Zhou Y, Plattner JJ, Baker SJ, Liu L, Bu W, Kazmierski WM, Wright LL, Smith GK, Jarvest RL, Duan M, Ji JJ, Cooper JP, Tallant MD, Crosby RM, Creech K, Ni ZJ, Zou W, Wright J.

Bioorg Med Chem Lett. 2010 Dec 15;20(24):7493-7. doi: 10.1016/j.bmcl.2010.10.007. Epub 2010 Oct 30.

PMID:
21041080
9.

Investigation of glycine alpha-ketoamide HCV NS3 protease inhibitors: effect of carboxylic acid isosteres.

Han W, Jiang X, Hu Z, Wasserman ZR, Decicco CP.

Bioorg Med Chem Lett. 2005 Aug 1;15(15):3487-90.

PMID:
15982872
10.

Novel potent hepatitis C virus NS3 serine protease inhibitors derived from proline-based macrocycles.

Chen KX, Njoroge FG, Arasappan A, Venkatraman S, Vibulbhan B, Yang W, Parekh TN, Pichardo J, Prongay A, Cheng KC, Butkiewicz N, Yao N, Madison V, Girijavallabhan V.

J Med Chem. 2006 Feb 9;49(3):995-1005.

PMID:
16451065
11.

Design and synthesis of potent, non-peptide inhibitors of HCV NS3 protease.

Zhang X, Schmitt AC, Jiang W, Wasserman Z, Decicco CP.

Bioorg Med Chem Lett. 2003 Mar 24;13(6):1157-60.

PMID:
12643933
12.

Discovery of achiral inhibitors of the hepatitis C virus NS3 protease based on 2(1H)-pyrazinones.

Ortqvist P, Gising J, Ehrenberg AE, Vema A, Borg A, Karlén A, Larhed M, Danielson UH, Sandström A.

Bioorg Med Chem. 2010 Sep 1;18(17):6512-25. doi: 10.1016/j.bmc.2010.06.101. Epub 2010 Jul 3.

PMID:
20673728
13.

Phenylglycine as a novel P2 scaffold in hepatitis C virus NS3 protease inhibitors.

Ortqvist P, Peterson SD, Kerblom E, Gossas T, Sabnis YA, Fransson R, Lindeberg G, Helena Danielson U, Karlén A, Sandström A.

Bioorg Med Chem. 2007 Feb 1;15(3):1448-74. Epub 2006 Nov 6.

PMID:
17113777
14.

The Journey to the Discovery of Boceprevir: an NS3-NS4 HCV protease inhibitor for the treatment of chronic hepatitis C.

Chen KX, Njoroge FG.

Prog Med Chem. 2010;49:1-36. doi: 10.1016/S0079-6468(10)49001-3. Review. No abstract available.

PMID:
20855037
15.

Discovery of novel P2 substituted 4-biaryl proline inhibitors of hepatitis C virus NS3 serine protease.

Bailey MD, Halmos T, Lemke CT.

Bioorg Med Chem Lett. 2013 Aug 1;23(15):4436-40. doi: 10.1016/j.bmcl.2013.05.046. Epub 2013 May 22.

PMID:
23773864
16.

Potent ketoamide inhibitors of HCV NS3 protease derived from quaternized P1 groups.

Venkatraman S, Velazquez F, Wu W, Blackman M, Madison V, Njoroge FG.

Bioorg Med Chem Lett. 2010 Apr 1;20(7):2151-5. doi: 10.1016/j.bmcl.2010.02.051. Epub 2010 Feb 14.

PMID:
20226659
17.

Pyrrolidine-5,5-trans-lactams. 1. Synthesis and incorporation into inhibitors of hepatitis C virus NS3/4A protease.

Andrews DM, Carey SJ, Chaignot H, Coomber BA, Gray NM, Hind SL, Jones PS, Mills G, Robinson JE, Slater MJ.

Org Lett. 2002 Dec 12;4(25):4475-8.

PMID:
12465916
18.

Synthesis and SAR of potent inhibitors of the Hepatitis C virus NS3/4A protease: exploration of P2 quinazoline substituents.

Nilsson M, Belfrage AK, Lindström S, Wähling H, Lindquist C, Ayesa S, Kahnberg P, Pelcman M, Benkestock K, Agback T, Vrang L, Terelius Y, Wikström K, Hamelink E, Rydergård C, Edlund M, Eneroth A, Raboisson P, Lin TI, de Kock H, Wigerinck P, Simmen K, Samuelsson B, Rosenquist S.

Bioorg Med Chem Lett. 2010 Jul 15;20(14):4004-11. doi: 10.1016/j.bmcl.2010.05.029. Epub 2010 May 21.

PMID:
20541405
19.

Towards the second generation of Boceprevir: Dithianes as an alternative P2 substituent for 2,2-dimethyl cycloproyl proline in HCV NS3 protease inhibitors.

Nair LG, Bogen S, Ruan S, Pan W, Pike R, Tong X, Cheng KC, Guo Z, Doll RJ, Njoroge FG.

Bioorg Med Chem Lett. 2010 Mar 1;20(5):1689-92. doi: 10.1016/j.bmcl.2010.01.037. Epub 2010 Jan 20.

PMID:
20149655
20.

Discovery of the HCV NS3/4A protease inhibitor (1R,5S)-N-[3-amino-1-(cyclobutylmethyl)-2,3-dioxopropyl]-3- [2(S)-[[[(1,1-dimethylethyl)amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]- 6,6-dimethyl-3-azabicyclo[3.1.0]hexan-2(S)-carboxamide (Sch 503034) II. Key steps in structure-based optimization.

Prongay AJ, Guo Z, Yao N, Pichardo J, Fischmann T, Strickland C, Myers J Jr, Weber PC, Beyer BM, Ingram R, Hong Z, Prosise WW, Ramanathan L, Taremi SS, Yarosh-Tomaine T, Zhang R, Senior M, Yang RS, Malcolm B, Arasappan A, Bennett F, Bogen SL, Chen K, Jao E, Liu YT, Lovey RG, Saksena AK, Venkatraman S, Girijavallabhan V, Njoroge FG, Madison V.

J Med Chem. 2007 May 17;50(10):2310-8. Epub 2007 Apr 20.

PMID:
17444623
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