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Items: 1 to 20 of 203

1.

5,5'- and 6,6'-dialkyl-5,6-dihydro-1H-pyridin-2-ones as potent inhibitors of HCV NS5B polymerase.

Ellis DA, Blazel JK, Tran CV, Ruebsam F, Murphy DE, Li LS, Zhao J, Zhou Y, McGuire HM, Xiang AX, Webber SE, Zhao Q, Han Q, Kissinger CR, Lardy M, Gobbi A, Showalter RE, Shah AM, Tsan M, Patel RA, LeBrun LA, Kamran R, Bartkowski DM, Nolan TG, Norris DA, Sergeeva MV, Kirkovsky L.

Bioorg Med Chem Lett. 2009 Nov 1;19(21):6047-52. doi: 10.1016/j.bmcl.2009.09.051. Epub 2009 Sep 17.

PMID:
19796938
2.

2-(3-Thienyl)-5,6-dihydroxypyrimidine-4-carboxylic acids as inhibitors of HCV NS5B RdRp.

Pacini B, Avolio S, Ercolani C, Koch U, Migliaccio G, Narjes F, Pacini L, Tomei L, Harper S.

Bioorg Med Chem Lett. 2009 Nov 1;19(21):6245-9. doi: 10.1016/j.bmcl.2009.06.106. Epub 2009 Jul 17.

PMID:
19800789
3.

Discovery of 4H-pyrazolo[1,5-a]pyrimidin-7-ones as potent inhibitors of hepatitis C virus polymerase.

Deng Y, Shipps GW Jr, Wang T, Popovici-Muller J, Rosner KE, Siddiqui MA, Duca J, Cooper AB, Cable M.

Bioorg Med Chem Lett. 2009 Sep 15;19(18):5363-7. doi: 10.1016/j.bmcl.2009.07.124. Epub 2009 Aug 6.

PMID:
19682898
4.

Non-nucleoside inhibitors of the hepatitis C virus NS5B polymerase: discovery and preliminary SAR of benzimidazole derivatives.

Beaulieu PL, Bös M, Bousquet Y, Fazal G, Gauthier J, Gillard J, Goulet S, LaPlante S, Poupart MA, Lefebvre S, McKercher G, Pellerin C, Austel V, Kukolj G.

Bioorg Med Chem Lett. 2004 Jan 5;14(1):119-24.

PMID:
14684311
5.

Identification of N,N-disubstituted phenylalanines as a novel class of inhibitors of hepatitis C NS5B polymerase.

Chan L, Reddy TJ, Proulx M, Das SK, Pereira O, Wang W, Siddiqui A, Yannopoulos CG, Poisson C, Turcotte N, Drouin A, Alaoui-Ismaili MH, Bethell R, Hamel M, L'Heureux L, Bilimoria D, Nguyen-Ba N.

J Med Chem. 2003 Apr 10;46(8):1283-5.

PMID:
12672227
6.

5,6-Dihydro-1H-pyridin-2-ones as potent inhibitors of HCV NS5B polymerase.

Ruebsam F, Tran CV, Li LS, Kim SH, Xiang AX, Zhou Y, Blazel JK, Sun Z, Dragovich PS, Zhao J, McGuire HM, Murphy DE, Tran MT, Stankovic N, Ellis DA, Gobbi A, Showalter RE, Webber SE, Shah AM, Tsan M, Patel RA, Lebrun LA, Hou HJ, Kamran R, Sergeeva MV, Bartkowski DM, Nolan TG, Norris DA, Kirkovsky L.

Bioorg Med Chem Lett. 2009 Jan 15;19(2):451-8. doi: 10.1016/j.bmcl.2008.11.048. Epub 2008 Nov 18.

PMID:
19054673
7.

Parallel synthesis of 5-cyano-6-aryl-2-thiouracil derivatives as inhibitors for hepatitis C viral NS5B RNA-dependent RNA polymerase.

Ding Y, Girardet JL, Smith KL, Larson G, Prigaro B, Wu JZ, Yao N.

Bioorg Chem. 2006 Feb;34(1):26-38. Epub 2005 Dec 19.

PMID:
16360193
8.

Quinolones as HCV NS5B polymerase inhibitors.

Kumar DV, Rai R, Brameld KA, Somoza JR, Rajagopalan R, Janc JW, Xia YM, Ton TL, Shaghafi MB, Hu H, Lehoux I, To N, Young WB, Green MJ.

Bioorg Med Chem Lett. 2011 Jan 1;21(1):82-7. doi: 10.1016/j.bmcl.2010.11.068. Epub 2010 Nov 21.

PMID:
21145235
9.

Novel HCV NS5B polymerase inhibitors derived from 4-(1',1'-dioxo-1',4'-dihydro-1'lambda(6)-benzo[1',2',4']thiadiazin-3'-yl)-5-hydroxy-2H-pyridazin-3-ones. Part 2: Variation of the 2- and 6-pyridazinone substituents.

Zhou Y, Li LS, Dragovich PS, Murphy DE, Tran CV, Ruebsam F, Webber SE, Shah AM, Tsan M, Averill A, Showalter RE, Patel R, Han Q, Zhao Q, Hermann T, Kissinger CR, Lebrun L, Sergeeva MV.

Bioorg Med Chem Lett. 2008 Feb 15;18(4):1419-24. doi: 10.1016/j.bmcl.2008.01.005. Epub 2008 Jan 8.

PMID:
18226901
10.

Ligand-induced changes in hepatitis C virus NS5B polymerase structure.

Rigat K, Wang Y, Hudyma TW, Ding M, Zheng X, Gentles RG, Beno BR, Gao M, Roberts SB.

Antiviral Res. 2010 Nov;88(2):197-206. doi: 10.1016/j.antiviral.2010.08.014. Epub 2010 Sep 9.

PMID:
20813137
11.

The discovery and structure-activity relationships of pyrano[3,4-b]indole based inhibitors of hepatitis C virus NS5B polymerase.

LaPorte MG, Draper TL, Miller LE, Blackledge CW, Leister LK, Amparo E, Hussey AR, Young DC, Chunduru SK, Benetatos CA, Rhodes G, Gopalsamy A, Herbertz T, Burns CJ, Condon SM.

Bioorg Med Chem Lett. 2010 May 1;20(9):2968-73. doi: 10.1016/j.bmcl.2010.03.002. Epub 2010 Mar 6.

PMID:
20347591
12.

Novel HCV NS5B polymerase inhibitors derived from 4-(1',1'-dioxo-1',4'-dihydro-1'lambda6-benzo[1',2',4']thiadiazin-3'-yl)-5-hydroxy-2H-pyridazin-3-ones. Part 1: exploration of 7'-substitution of benzothiadiazine.

Zhou Y, Webber SE, Murphy DE, Li LS, Dragovich PS, Tran CV, Sun Z, Ruebsam F, Shah AM, Tsan M, Showalter RE, Patel R, Li B, Zhao Q, Han Q, Hermann T, Kissinger CR, Lebrun L, Sergeeva MV, Kirkovsky L.

Bioorg Med Chem Lett. 2008 Feb 15;18(4):1413-8. doi: 10.1016/j.bmcl.2008.01.007. Epub 2008 Jan 8.

PMID:
18242088
13.

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
14.

Non-nucleoside inhibitors of HCV NS5B polymerase. Part 1: Synthetic and computational exploration of the binding modes of benzothiadiazine and 1,4-benzothiazine HCV NS5b polymerase inhibitors.

Hendricks RT, Fell JB, Blake JF, Fischer JP, Robinson JE, Spencer SR, Stengel PJ, Bernacki AL, Leveque VJ, Le Pogam S, Rajyaguru S, Najera I, Josey JA, Harris JR, Swallow S.

Bioorg Med Chem Lett. 2009 Jul 1;19(13):3637-41. doi: 10.1016/j.bmcl.2009.04.119. Epub 2009 May 3.

PMID:
19447623
15.

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
16.

Structure-based design of a benzodiazepine scaffold yields a potent allosteric inhibitor of hepatitis C NS5B RNA polymerase.

Vandyck K, Cummings MD, Nyanguile O, Boutton CW, Vendeville S, McGowan D, Devogelaere B, Amssoms K, Last S, Rombauts K, Tahri A, Lory P, Hu L, Beauchamp DA, Simmen K, Raboisson P.

J Med Chem. 2009 Jul 23;52(14):4099-102. doi: 10.1021/jm9005548.

PMID:
19507864
17.

Non-nucleoside inhibitors of the hepatitis C virus NS5B polymerase: discovery of benzimidazole 5-carboxylic amide derivatives with low-nanomolar potency.

Beaulieu PL, Bös M, Bousquet Y, DeRoy P, Fazal G, Gauthier J, Gillard J, Goulet S, McKercher G, Poupart MA, Valois S, Kukolj G.

Bioorg Med Chem Lett. 2004 Feb 23;14(4):967-71.

PMID:
15013003
18.

Further SAR studies on novel small molecule inhibitors of the hepatitis C (HCV) NS5B polymerase.

Reddy TJ, Chan L, Turcotte N, Proulx M, Pereira OZ, Das SK, Siddiqui A, Wang W, Poisson C, Yannopoulos CG, Bilimoria D, L'Heureux L, Alaoui HM, Nguyen-Ba N.

Bioorg Med Chem Lett. 2003 Oct 6;13(19):3341-4.

PMID:
12951122
19.

A homogeneous, solid-phase assay for hepatitis C virus RNA-dependent RNA polymerase.

Wang YK, Rigat KL, Roberts SB, Gao M.

Anal Biochem. 2006 Dec 1;359(1):106-11. Epub 2006 Oct 4.

PMID:
17054898
20.

Novel HCV NS5B polymerase inhibitors derived from 4-(1',1'-dioxo-1',4'-dihydro-1'lambda(6)-benzo[1',2',4']thiadiazin-3'-yl)-5-hydroxy-2H-pyridazin-3-ones. Part 5: Exploration of pyridazinones containing 6-amino-substituents.

Dragovich PS, Blazel JK, Ellis DA, Han Q, Kamran R, Kissinger CR, LeBrun LA, Li LS, Murphy DE, Noble M, Patel RA, Ruebsam F, Sergeeva MV, Shah AM, Showalter RE, Tran CV, Tsan M, Webber SE, Kirkovsky L, Zhou Y.

Bioorg Med Chem Lett. 2008 Oct 15;18(20):5635-9. doi: 10.1016/j.bmcl.2008.08.094. Epub 2008 Aug 29.

PMID:
18796353

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