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Items: 1 to 20 of 121

1.

Probing the cation binding modes of macrocyclic HCV protease inhibitor BILN 2061 by multinuclear NMR.

Busacca CA, Jones PJ, Campbell SJ, Saha AK, Gonnella NC, Senanayake CH.

J Pharm Biomed Anal. 2012 Nov;70:609-13. doi: 10.1016/j.jpba.2012.06.013. Epub 2012 Jun 15.

PMID:
22766359
2.

Synthesis of BILN 2061, an HCV NS3 protease inhibitor with proven antiviral effect in humans.

Faucher AM, Bailey MD, Beaulieu PL, Brochu C, Duceppe JS, Ferland JM, Ghiro E, Gorys V, Halmos T, Kawai SH, Poirier M, Simoneau B, Tsantrizos YS, Llinàs-Brunet M.

Org Lett. 2004 Aug 19;6(17):2901-4.

PMID:
15330643
3.

Bismacrocyclic inhibitors of hepatitis C NS3/4a protease.

McCauley JA, Rudd MT, Nguyen KT, McIntyre CJ, Romano JJ, Bush KJ, Varga SL, Ross CW 3rd, Carroll SS, DiMuzio J, Stahlhut MW, Olsen DB, Lyle TA, Vacca JP, Liverton NJ.

Angew Chem Int Ed Engl. 2008;47(47):9104-7. doi: 10.1002/anie.200803298. No abstract available.

PMID:
18925594
5.

Efficient large-scale synthesis of BILN 2061, a potent HCV protease inhibitor, by a convergent approach based on ring-closing metathesis.

Yee NK, Farina V, Houpis IN, Haddad N, Frutos RP, Gallou F, Wang XJ, Wei X, Simpson RD, Feng X, Fuchs V, Xu Y, Tan J, Zhang L, Xu J, Smith-Keenan LL, Vitous J, Ridges MD, Spinelli EM, Johnson M, Donsbach K, Nicola T, Brenner M, Winter E, Kreye P, Samstag W.

J Org Chem. 2006 Sep 15;71(19):7133-45.

PMID:
16958506
6.

Development of hepatitis C virus chimeric replicons for identifying broad spectrum NS3 protease inhibitors.

Binder J, Tetangco S, Weinshank M, Maegley K, Lingardo L, Diehl W, Love R, Patick AK, Smith GJ 3rd.

Antiviral Res. 2011 Aug;91(2):102-11. doi: 10.1016/j.antiviral.2011.05.007. Epub 2011 May 19.

PMID:
21620899
7.

Resistance of hepatitis C virus to NS3-4A protease inhibitors: mechanisms of drug resistance induced by R155Q, A156T, D168A and D168V mutations.

Courcambeck J, Bouzidi M, Perbost R, Jouirou B, Amrani N, Cacoub P, Pèpe G, Sabatier JM, Halfon P.

Antivir Ther. 2006;11(7):847-55.

PMID:
17302247
8.

RCM macrocyclization made practical: an efficient synthesis of HCV protease inhibitor BILN 2061.

Shu C, Zeng X, Hao MH, Wei X, Yee NK, Busacca CA, Han Z, Farina V, Senanayake CH.

Org Lett. 2008 Mar 20;10(6):1303-6. doi: 10.1021/ol800183x. Epub 2008 Feb 23.

PMID:
18293994
9.

Accounting for strain variations and resistance mutations in the characterization of hepatitis C NS3 protease inhibitors.

Ehrenberg AE, Schmuck B, Anwar MI, Gustafsson SS, Stenberg G, Danielson UH.

J Enzyme Inhib Med Chem. 2014 Dec;29(6):868-76. doi: 10.3109/14756366.2013.864651. Epub 2014 Feb 11.

PMID:
24517372
10.

Synthesis, antiviral activity, and conformational studies of a P3 aza-peptide analog of a potent macrocyclic tripeptide HCV protease inhibitor.

Randolph JT, Zhang X, Huang PP, Klein LL, Kurtz KA, Konstantinidis AK, He W, Kati WM, Kempf DJ.

Bioorg Med Chem Lett. 2008 Apr 15;18(8):2745-50. doi: 10.1016/j.bmcl.2008.02.053. Epub 2008 Feb 26.

PMID:
18375121
11.

Mechanistic and kinetic characterization of hepatitis C virus NS3 protein interactions with NS4A and protease inhibitors.

Geitmann M, Dahl G, Danielson UH.

J Mol Recognit. 2011 Jan-Feb;24(1):60-70. doi: 10.1002/jmr.1023.

PMID:
21194118
12.

Discovery of novel potent and selective dipeptide hepatitis C virus NS3/4A serine protease inhibitors.

Raboisson P, Lin TI, Kock Hd, Vendeville S, Vreken WV, McGowan D, Tahri A, Hu L, Lenz O, Delouvroy F, Surleraux D, Wigerinck P, Nilsson M, Rosenquist S, Samuelsson B, Simmen K.

Bioorg Med Chem Lett. 2008 Sep 15;18(18):5095-100. doi: 10.1016/j.bmcl.2008.07.124. Epub 2008 Aug 3.

PMID:
18722116
13.

An NS3 protease inhibitor with antiviral effects in humans infected with hepatitis C virus.

Lamarre D, Anderson PC, Bailey M, Beaulieu P, Bolger G, Bonneau P, Bös M, Cameron DR, Cartier M, Cordingley MG, Faucher AM, Goudreau N, Kawai SH, Kukolj G, Lagacé L, LaPlante SR, Narjes H, Poupart MA, Rancourt J, Sentjens RE, St George R, Simoneau B, Steinmann G, Thibeault D, Tsantrizos YS, Weldon SM, Yong CL, Llinàs-Brunet M.

Nature. 2003 Nov 13;426(6963):186-9. Epub 2003 Oct 26. Erratum in: Nature. 2003 Nov 20;246.

14.

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
15.

Mapping natural polymorphisms of hepatitis C virus NS3/4A protease and antiviral resistance to inhibitors in worldwide isolates.

López-Labrador FX, Moya A, Gonzàlez-Candelas F.

Antivir Ther. 2008;13(4):481-94.

PMID:
18672527
16.

Protease and helicase activities of hepatitis C virus genotype 4, 5, and 6 NS3-NS4A proteins.

Massariol MJ, Zhao S, Marquis M, Thibeault D, White PW.

Biochem Biophys Res Commun. 2010 Jan 1;391(1):692-7. doi: 10.1016/j.bbrc.2009.11.122. Epub 2009 Nov 26.

PMID:
19944069
17.

In vitro studies of cross-resistance mutations against two hepatitis C virus serine protease inhibitors, VX-950 and BILN 2061.

Lin C, Gates CA, Rao BG, Brennan DL, Fulghum JR, Luong YP, Frantz JD, Lin K, Ma S, Wei YY, Perni RB, Kwong AD.

J Biol Chem. 2005 Nov 4;280(44):36784-91. Epub 2005 Aug 8.

18.

Novel macrocyclic inhibitors of hepatitis C NS3/4A protease featuring a 2-amino-1,3-thiazole as a P4 carbamate replacement.

Di Francesco ME, Dessole G, Nizi E, Pace P, Koch U, Fiore F, Pesci S, Di Muzio J, Monteagudo E, Rowley M, Summa V.

J Med Chem. 2009 Nov 26;52(22):7014-28. doi: 10.1021/jm900524b.

PMID:
19856919
19.

Virology: fresh assault on hepatitis C.

Rice CM.

Nature. 2003 Nov 13;426(6963):129-31. No abstract available.

PMID:
14578912
20.

Synthesis and biological evaluations of P4-benzoxaborole-substituted macrocyclic inhibitors of HCV NS3 protease.

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

Bioorg Med Chem Lett. 2010 Dec 15;20(24):7317-22. doi: 10.1016/j.bmcl.2010.10.071. Epub 2010 Oct 21.

PMID:
21067923

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