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Items: 1 to 20 of 121

1.

Discovery of novel dialkyl substituted thiophene inhibitors of HCV by in silico screening of the NS5B RdRp.

Louise-May S, Yang W, Nie X, Liu D, Deshpande MS, Phadke AS, Huang M, Agarwal A.

Bioorg Med Chem Lett. 2007 Jul 15;17(14):3905-9. Epub 2007 May 3.

PMID:
17512198
2.

Discovery of thiophene-2-carboxylic acids as potent inhibitors of HCV NS5B polymerase and HCV subgenomic RNA replication. Part 1: Sulfonamides.

Chan L, Das SK, Reddy TJ, Poisson C, Proulx M, Pereira O, Courchesne M, Roy C, Wang W, Siddiqui A, Yannopoulos CG, Nguyen-Ba N, Labrecque D, Bethell R, Hamel M, Courtemanche-Asselin P, L'Heureux L, David M, Nicolas O, Brunette S, Bilimoria D, Bédard J.

Bioorg Med Chem Lett. 2004 Feb 9;14(3):793-6.

PMID:
14741291
3.

Discovery of thiophene-2-carboxylic acids as potent inhibitors of HCV NS5B polymerase and HCV subgenomic RNA replication. Part 2: tertiary amides.

Chan L, Pereira O, Reddy TJ, Das SK, Poisson C, Courchesne M, Proulx M, Siddiqui A, Yannopoulos CG, Nguyen-Ba N, Roy C, Nasturica D, Moinet C, Bethell R, Hamel M, L'Heureux L, David M, Nicolas O, Courtemanche-Asselin P, Brunette S, Bilimoria D, Bédard J.

Bioorg Med Chem Lett. 2004 Feb 9;14(3):797-800.

PMID:
14741292
4.

Tetrahydrobenzothiophene inhibitors of hepatitis C virus NS5B polymerase.

Laporte MG, Lessen TA, Leister L, Cebzanov D, Amparo E, Faust C, Ortlip D, Bailey TR, Nitz TJ, Chunduru SK, Young DC, Burns CJ.

Bioorg Med Chem Lett. 2006 Jan 1;16(1):100-3. Epub 2005 Nov 2.

PMID:
16260131
5.

2-(2-Thienyl)-5,6-dihydroxy-4-carboxypyrimidines as inhibitors of the hepatitis C virus NS5B polymerase: discovery, SAR, modeling, and mutagenesis.

Koch U, Attenni B, Malancona S, Colarusso S, Conte I, Di Filippo M, Harper S, Pacini B, Giomini C, Thomas S, Incitti I, Tomei L, De Francesco R, Altamura S, Matassa VG, Narjes F.

J Med Chem. 2006 Mar 9;49(5):1693-705.

PMID:
16509585
6.

Inhibitors of HCV NS5B polymerase: synthesis and structure-activity relationships of unsymmetrical 1-hydroxy-4,4-dialkyl-3-oxo-3,4-dihydronaphthalene benzothiadiazine derivatives.

Krueger AC, Madigan DL, Green BE, Hutchinson DK, Jiang WW, Kati WM, Liu Y, Maring CJ, Masse SV, McDaniel KF, Middleton TR, Mo H, Molla A, Montgomery DA, Ng TI, Kempf DJ.

Bioorg Med Chem Lett. 2007 Apr 15;17(8):2289-92. Epub 2007 Jan 27.

PMID:
17300933
7.

Identification of novel inhibitors of HCV RNA-dependent RNA polymerase by pharmacophore-based virtual screening and in vitro evaluation.

Ryu K, Kim ND, Choi SI, Han CK, Yoon JH, No KT, Kim KH, Seong BL.

Bioorg Med Chem. 2009 Apr 15;17(8):2975-82. doi: 10.1016/j.bmc.2009.03.024. Epub 2009 Mar 18.

PMID:
19332375
8.

Cyclic amide bioisosterism: strategic application to the design and synthesis of HCV NS5B polymerase inhibitors.

Yang H, Hendricks RT, Arora N, Nitzan D, Yee C, Lucas MC, Yang Y, Fung A, Rajyaguru S, Harris SF, Leveque VJ, Hang JQ, Pogam SL, Reuter D, Tavares GA.

Bioorg Med Chem Lett. 2010 Aug 1;20(15):4614-9. doi: 10.1016/j.bmcl.2010.06.008. Epub 2010 Jun 8.

PMID:
20584604
9.

Non-nucleoside inhibitors of HCV polymerase NS5B. Part 4: structure-based design, synthesis, and biological evaluation of benzo[d]isothiazole-1,1-dioxides.

de Vicente J, Hendricks RT, Smith DB, Fell JB, Fischer J, Spencer SR, Stengel PJ, Mohr P, Robinson JE, Blake JF, Hilgenkamp RK, Yee C, Adjabeng G, Elworthy TR, Li J, Wang B, Bamberg JT, Harris SF, Wong A, Leveque VJ, Najera I, Le Pogam S, Rajyaguru S, Ao-Ieong G, Alexandrova L, Larrabee S, Brandl M, Briggs A, Sukhtankar S, Farrell R.

Bioorg Med Chem Lett. 2009 Oct 1;19(19):5652-6. doi: 10.1016/j.bmcl.2009.08.022. Epub 2009 Aug 8.

PMID:
19709881
10.

Structure-based design, synthesis, and biological evaluation of 1,1-dioxoisothiazole and benzo[b]thiophene-1,1-dioxide derivatives as novel inhibitors of hepatitis C virus NS5B polymerase.

Kim SH, Tran MT, Ruebsam F, Xiang AX, Ayida B, McGuire H, Ellis D, Blazel J, Tran CV, Murphy DE, Webber SE, Zhou Y, Shah AM, Tsan M, Showalter RE, Patel R, Gobbi A, LeBrun LA, Bartkowski DM, Nolan TG, Norris DA, Sergeeva MV, Kirkovsky L, Zhao Q, Han Q, Kissinger CR.

Bioorg Med Chem Lett. 2008 Jul 15;18(14):4181-5. doi: 10.1016/j.bmcl.2008.05.083. Epub 2008 May 24.

PMID:
18554907
11.

HCV NS5B polymerase-bound conformation of a soluble sulfonamide inhibitor by 2D transferred NOESY.

Yannopoulos CG, Xu P, Ni F, Chan L, Pereira OZ, Reddy TJ, Das SK, Poisson C, Nguyen-Ba N, Turcotte N, Proulx M, Halab L, Wang W, Bédard J, Morin N, Hamel M, Nicolas O, Bilimoria D, L'Heureux L, Bethell R, Dionne G.

Bioorg Med Chem Lett. 2004 Nov 1;14(21):5333-7.

PMID:
15454222
12.

4-Thiazolidinones: a novel class of hepatitis C virus NS5B polymerase inhibitors.

Kaushik-Basu N, Bopda-Waffo A, Talele TT, Basu A, Chen Y, Kucukguzel SG.

Front Biosci. 2008 May 1;13:3857-68.

PMID:
18508480
13.

Identification and structure-based optimization of novel dihydropyrones as potent HCV RNA polymerase inhibitors.

Li H, Tatlock J, Linton A, Gonzalez J, Borchardt A, Dragovich P, Jewell T, Prins T, Zhou R, Blazel J, Parge H, Love R, Hickey M, Doan C, Shi S, Duggal R, Lewis C, Fuhrman S.

Bioorg Med Chem Lett. 2006 Sep 15;16(18):4834-8. Epub 2006 Jul 7.

PMID:
16824756
14.

Active site inhibitors of HCV NS5B polymerase. The development and pharmacophore of 2-thienyl-5,6-dihydroxypyrimidine-4-carboxylic acid.

Stansfield I, Avolio S, Colarusso S, Gennari N, Narjes F, Pacini B, Ponzi S, Harper S.

Bioorg Med Chem Lett. 2004 Oct 18;14(20):5085-8.

PMID:
15380204
15.

HCV NS5b RNA-dependent RNA polymerase inhibitors: from alpha,gamma-diketoacids to 4,5-dihydroxypyrimidine- or 3-methyl-5-hydroxypyrimidinonecarboxylic acids. Design and synthesis.

Summa V, Petrocchi A, Matassa VG, Taliani M, Laufer R, De Francesco R, Altamura S, Pace P.

J Med Chem. 2004 Oct 21;47(22):5336-9.

PMID:
15481971
16.

Non-nucleoside inhibitors of HCV polymerase NS5B. Part 2: Synthesis and structure-activity relationships of benzothiazine-substituted quinolinediones.

de Vicente J, Hendricks RT, Smith DB, Fell JB, Fischer J, Spencer SR, Stengel PJ, Mohr P, Robinson JE, Blake JF, Hilgenkamp RK, Yee C, Adjabeng G, Elworthy TR, Tracy J, Chin E, Li J, Wang B, Bamberg JT, Stephenson R, Oshiro C, Harris SF, Ghate M, Leveque V, Najera I, Le Pogam S, Rajyaguru S, Ao-Ieong G, Alexandrova L, Larrabee S, Brandl M, Briggs A, Sukhtankar S, Farrell R, Xu B.

Bioorg Med Chem Lett. 2009 Jul 1;19(13):3642-6. doi: 10.1016/j.bmcl.2009.05.004. Epub 2009 May 7.

PMID:
19457662
17.
19.

Structure-activity relationship (SAR) studies of quinoxalines as novel HCV NS5B RNA-dependent RNA polymerase inhibitors.

Rong F, Chow S, Yan S, Larson G, Hong Z, Wu J.

Bioorg Med Chem Lett. 2007 Mar 15;17(6):1663-6. Epub 2007 Jan 8.

PMID:
17258458
20.

Non-nucleoside inhibitors of HCV polymerase NS5B. Part 3: synthesis and optimization studies of benzothiazine-substituted tetramic acids.

de Vicente J, Hendricks RT, Smith DB, Fell JB, Fischer J, Spencer SR, Stengel PJ, Mohr P, Robinson JE, Blake JF, Hilgenkamp RK, Yee C, Zhao J, Elworthy TR, Tracy J, Chin E, Li J, Lui A, Wang B, Oshiro C, Harris SF, Ghate M, Leveque VJ, Najera I, Le Pogam S, Rajyaguru S, Ao-Ieong G, Alexandrova L, Fitch B, Brandl M, Masjedizadeh M, Wu SY, de Keczer S, Voronin T.

Bioorg Med Chem Lett. 2009 Oct 1;19(19):5648-51. doi: 10.1016/j.bmcl.2009.08.023. Epub 2009 Aug 8.

PMID:
19700319

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