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Results: 1 to 20 of 223

1.

Hepatitis C virus NS3-4A serine protease inhibitors: SAR of P'2 moiety with improved potency.

Arasappan A, Njoroge FG, Chan TY, Bennett F, Bogen SL, Chen K, Gu H, Hong L, Jao E, Liu YT, Lovey RG, Parekh T, Pike RE, Pinto P, Santhanam B, Venkatraman S, Vaccaro H, Wang H, Yang X, Zhu Z, Mckittrick B, Saksena AK, Girijavallabhan V, Pichardo J, Butkiewicz N, Ingram R, Malcolm B, Prongay A, Yao N, Marten B, Madison V, Kemp S, Levy O, Lim-Wilby M, Tamura S, Ganguly AK.

Bioorg Med Chem Lett. 2005 Oct 1;15(19):4180-4.

PMID:
16087332
[PubMed - indexed for MEDLINE]
2.

Depeptidization efforts on P3-P2' alpha-ketoamide inhibitors of HCV NS3-4A serine protease: effect on HCV replicon activity.

Bogen SL, Ruan S, Liu R, Agrawal S, Pichardo J, Prongay A, Baroudy B, Saksena AK, Girijavallabhan V, Njoroge FG.

Bioorg Med Chem Lett. 2006 Mar 15;16(6):1621-7. Epub 2006 Jan 4.

PMID:
16387495
[PubMed - indexed for MEDLINE]
3.

Novel inhibitors of hepatitis C NS3-NS4A serine protease derived from 2-aza-bicyclo[2.2.1]heptane-3-carboxylic acid.

Venkatraman S, Njoroge FG, Wu W, Girijavallabhan V, Prongay AJ, Butkiewicz N, Pichardo J.

Bioorg Med Chem Lett. 2006 Mar 15;16(6):1628-32. Epub 2006 Jan 18.

PMID:
16413182
[PubMed - indexed for MEDLINE]
4.

Inhibitors of hepatitis C virus NS3.4A protease 2. Warhead SAR and optimization.

Perni RB, Pitlik J, Britt SD, Court JJ, Courtney LF, Deininger DD, Farmer LJ, Gates CA, Harbeson SL, Levin RB, Lin C, Lin K, Moon YC, Luong YP, O'Malley ET, Rao BG, Thomson JA, Tung RD, Van Drie JH, Wei Y.

Bioorg Med Chem Lett. 2004 Mar 22;14(6):1441-6.

PMID:
15006379
[PubMed - indexed for MEDLINE]
5.

Potent 7-hydroxy-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid-based macrocyclic inhibitors of hepatitis C virus NS3 protease.

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

J Med Chem. 2006 Jan 26;49(2):567-74.

PMID:
16420042
[PubMed - indexed for MEDLINE]
6.

Hepatitis C virus NS3-4A serine protease inhibitors: use of a P2-P1 cyclopropyl alanine combination for improved potency.

Bogen S, Saksena AK, Arasappan A, Gu H, Njoroge FG, Girijavallabhan V, Pichardo J, Butkiewicz N, Prongay A, Madison V.

Bioorg Med Chem Lett. 2005 Oct 15;15(20):4515-9.

PMID:
16112862
[PubMed - indexed for MEDLINE]
7.

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
[PubMed - indexed for MEDLINE]
8.

Novel azapeptide inhibitors of hepatitis C virus serine protease.

Bailey MD, Halmos T, Goudreau N, Lescop E, Llinàs-Brunet M.

J Med Chem. 2004 Jul 15;47(15):3788-99.

PMID:
15239657
[PubMed - indexed for MEDLINE]
9.

Prime site binding inhibitors of a serine protease: NS3/4A of hepatitis C virus.

Ingallinella P, Fattori D, Altamura S, Steinkühler C, Koch U, Cicero D, Bazzo R, Cortese R, Bianchi E, Pessi A.

Biochemistry. 2002 Apr 30;41(17):5483-92.

PMID:
11969409
[PubMed - indexed for MEDLINE]
10.

Novel 2-oxoimidazolidine-4-carboxylic acid derivatives as hepatitis C virus NS3-4A serine protease inhibitors: synthesis, activity, and X-ray crystal structure of an enzyme inhibitor complex.

Arasappan A, Njoroge FG, Parekh TN, Yang X, Pichardo J, Butkiewicz N, Prongay A, Yao N, Girijavallabhan V.

Bioorg Med Chem Lett. 2004 Dec 6;14(23):5751-5.

PMID:
15501035
[PubMed - indexed for MEDLINE]
11.

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
[PubMed - indexed for MEDLINE]
12.

Potent inhibitors of the hepatitis C virus NS3 protease: use of a novel P2 cyclopentane-derived template.

Johansson PO, Bäck M, Kvarnström I, Jansson K, Vrang L, Hamelink E, Hallberg A, Rosenquist A, Samuelsson B.

Bioorg Med Chem. 2006 Aug 1;14(15):5136-51. Epub 2006 May 3.

PMID:
16675222
[PubMed - indexed for MEDLINE]
13.

Toward the back-up of boceprevir (SCH 503034): discovery of new extended P4-capped ketoamide inhibitors of hepatitis C virus NS3 serine protease with improved potency and pharmacokinetic profiles.

Bogen SL, Pan W, Ruan S, Nair LG, Arasappan A, Bennett F, Chen KX, Jao E, Venkatraman S, Vibulbhan B, Liu R, Cheng KC, Guo Z, Tong X, Saksena AK, Girijavallabhan V, Njoroge FG.

J Med Chem. 2009 Jun 25;52(12):3679-88. doi: 10.1021/jm801632a.

PMID:
19456105
[PubMed - indexed for MEDLINE]
14.

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
[PubMed - indexed for MEDLINE]
15.

Hepatitis C virus NS3/4A protease.

Kwong AD, Kim JL, Rao G, Lipovsek D, Raybuck SA.

Antiviral Res. 1999 Feb;41(1):67-84. Review.

PMID:
10321580
[PubMed - indexed for MEDLINE]
16.

Azapeptides as inhibitors of the hepatitis C virus NS3 serine protease.

Zhang R, Durkin JP, Windsor WT.

Bioorg Med Chem Lett. 2002 Apr 8;12(7):1005-8.

PMID:
11909704
[PubMed - indexed for MEDLINE]
17.

Enzymatic characterization of membrane-associated hepatitis C virus NS3-4A heterocomplex serine protease activity expressed in human cells.

Hamill P, Jean F.

Biochemistry. 2005 May 3;44(17):6586-96.

PMID:
15850392
[PubMed - indexed for MEDLINE]
18.

The design and enzyme-bound crystal structure of indoline based peptidomimetic inhibitors of hepatitis C virus NS3 protease.

Ontoria JM, Di Marco S, Conte I, Di Francesco ME, Gardelli C, Koch U, Matassa VG, Poma M, Steinkühler C, Volpari C, Harper S.

J Med Chem. 2004 Dec 16;47(26):6443-6.

PMID:
15588076
[PubMed - indexed for MEDLINE]
19.

Molecular modeling based approach to potent P2-P4 macrocyclic inhibitors of hepatitis C NS3/4A protease.

Liverton NJ, Holloway MK, McCauley JA, Rudd MT, Butcher JW, Carroll SS, DiMuzio J, Fandozzi C, Gilbert KF, Mao SS, McIntyre CJ, Nguyen KT, Romano JJ, Stahlhut M, Wan BL, Olsen DB, Vacca JP.

J Am Chem Soc. 2008 Apr 9;130(14):4607-9. doi: 10.1021/ja711120r. Epub 2008 Mar 14.

PMID:
18338894
[PubMed - indexed for MEDLINE]
20.

NMR line-broadening and transferred NOESY as a medicinal chemistry tool for studying inhibitors of the hepatitis C virus NS3 protease domain.

LaPlante SR, Aubry N, Bonneau PR, Kukolj G, Lamarre D, Lefebvre S, Li H, Llinàs-Brunet M, Plouffe C, Cameron DR.

Bioorg Med Chem Lett. 2000 Oct 16;10(20):2271-4.

PMID:
11055336
[PubMed - indexed for MEDLINE]

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