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Items: 1 to 20 of 129

1.

A highly convergent and efficient synthesis of a macrocyclic hepatitis C virus protease inhibitor BI 201302.

Wei X, Shu C, Haddad N, Zeng X, Patel ND, Tan Z, Liu J, Lee H, Shen S, Campbell S, Varsolona RJ, Busacca CA, Hossain A, Yee NK, Senanayake CH.

Org Lett. 2013 Mar 1;15(5):1016-9. doi: 10.1021/ol303498m. Epub 2013 Feb 13.

PMID:
23406520
2.

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
3.

Synthesis of the HCV protease inhibitor Vaniprevir (MK-7009) using ring-closing metathesis strategy.

Kong J, Chen CY, Balsells-Padros J, Cao Y, Dunn RF, Dolman SJ, Janey J, Li H, Zacuto MJ.

J Org Chem. 2012 Apr 20;77(8):3820-8. doi: 10.1021/jo3001595. Epub 2012 Apr 10.

PMID:
22458448
4.

Development of a practical, asymmetric synthesis of the hepatitis C virus protease inhibitor MK-5172.

Kuethe J, Zhong YL, Yasuda N, Beutner G, Linn K, Kim M, Marcune B, Dreher SD, Humphrey G, Pei T.

Org Lett. 2013 Aug 16;15(16):4174-7. doi: 10.1021/ol401864t. Epub 2013 Aug 6.

PMID:
23919347
5.

Macrocyclic inhibitors of the NS3 protease as potential therapeutic agents of hepatitis C virus infection.

Tsantrizos YS, Bolger G, Bonneau P, Cameron DR, Goudreau N, Kukolj G, LaPlante SR, Llinàs-Brunet M, Nar H, Lamarre D.

Angew Chem Int Ed Engl. 2003 Mar 28;42(12):1356-60. No abstract available.

PMID:
12671967
6.

Design, synthesis, and biological activity of m-tyrosine-based 16- and 17-membered macrocyclic inhibitors of hepatitis C virus NS3 serine protease.

Chen KX, Njoroge FG, Pichardo J, Prongay A, Butkiewicz N, Yao N, Madison V, Girijavallabhan V.

J Med Chem. 2005 Oct 6;48(20):6229-35.

PMID:
16190750
7.

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
8.

Synthesis of bis-macrocyclic HCV protease inhibitor MK-6325 via intramolecular sp²-sp³ Suzuki-Miyaura coupling and ring closing metathesis.

Li H, Scott JP, Chen CY, Journet M, Belyk K, Balsells J, Kosjek B, Baxter CA, Stewart GW, Wise C, Alam M, Song ZJ, Tan L.

Org Lett. 2015 Mar 20;17(6):1533-6. doi: 10.1021/acs.orglett.5b00418. Epub 2015 Mar 10.

PMID:
25754231
9.

A convergent synthesis of the fully elaborated macrocyclic core of TMC-95A.

Coste A, Bayle A, Marrot J, Evano G.

Org Lett. 2014 Mar 7;16(5):1306-9. doi: 10.1021/ol403675c. Epub 2014 Feb 21.

PMID:
24559256
10.

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
11.

Design and synthesis of depeptidized macrocyclic inhibitors of hepatitis C NS3-4A protease using structure-based drug design.

Venkatraman S, Njoroge FG, Girijavallabhan VM, Madison VS, Yao NH, Prongay AJ, Butkiewicz N, Pichardo J.

J Med Chem. 2005 Aug 11;48(16):5088-91.

PMID:
16078825
12.

Pyrrolidine-5,5-trans-lactams. 4. Incorporation of a P3/P4 urea leads to potent intracellular inhibitors of hepatitis C virus NS3/4A protease.

Slater MJ, Amphlett EM, Andrews DM, Bamborough P, Carey SJ, Johnson MR, Jones PS, Mills G, Parry NR, Somers DO, Stewart AJ, Skarzynski T.

Org Lett. 2003 Nov 27;5(24):4627-30.

PMID:
14627400
13.

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
14.

Synergy of a hepatitis C virus (HCV) NS4A antagonist in combination with HCV protease and polymerase inhibitors.

Wyles DL, Kaihara KA, Schooley RT.

Antimicrob Agents Chemother. 2008 May;52(5):1862-4. doi: 10.1128/AAC.01208-07. Epub 2008 Mar 10.

15.

P2-P1' macrocyclization of P2 phenylglycine based HCV NS3 protease inhibitors using ring-closing metathesis.

Lampa A, Ehrenberg AE, Vema A, Åkerblom E, Lindeberg G, Danielson UH, Karlén A, Sandström A.

Bioorg Med Chem. 2011 Aug 15;19(16):4917-27. doi: 10.1016/j.bmc.2011.06.064. Epub 2011 Jun 28.

PMID:
21782454
16.

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
17.

Novel potent inhibitors of hepatitis C virus (HCV) NS3 protease with cyclic sulfonyl P3 cappings.

Chen KX, Vibulbhan B, Yang W, Nair LG, Tong X, Cheng KC, Njoroge FG.

Bioorg Med Chem Lett. 2009 Feb 15;19(4):1105-9. doi: 10.1016/j.bmcl.2008.12.111. Epub 2009 Jan 8.

PMID:
19168351
18.

A highly concise and convergent synthesis of HCV polymerase inhibitor Deleobuvir (BI 207127): application of a one-pot borylation-Suzuki coupling reaction.

Zhang Y, Lu BZ, Li G, Rodriguez S, Tan J, Wei HX, Liu J, Roschangar F, Ding F, Zhao W, Qu B, Reeves D, Grinberg N, Lee H, Heckmann G, Niemeier O, Brenner M, Tsantrizos Y, Beaulieu PL, Hossain A, Yee N, Farina V, Senanayake CH.

Org Lett. 2014 Sep 5;16(17):4558-61. doi: 10.1021/ol5021114. Epub 2014 Aug 8.

PMID:
25105303
19.

Synthesis and biological activity of macrocyclic inhibitors of hepatitis C virus (HCV) NS3 protease.

Chen KX, Njoroge FG, Prongay A, Pichardo J, Madison V, Girijavallabhan V.

Bioorg Med Chem Lett. 2005 Oct 15;15(20):4475-8.

PMID:
16112859
20.

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

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