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Results: 1 to 20 of 341

1.

Pyrrolo[1,2-b]pyridazin-2-ones as potent inhibitors of HCV NS5B polymerase.

Ruebsam F, Webber SE, Tran MT, Tran CV, Murphy DE, Zhao J, Dragovich PS, Kim SH, Li LS, Zhou Y, Han Q, Kissinger CR, Showalter RE, Lardy M, Shah AM, Tsan M, Patel R, Lebrun LA, Kamran R, Sergeeva MV, Bartkowski DM, Nolan TG, Norris DA, Kirkovsky L.

Bioorg Med Chem Lett. 2008 Jun 15;18(12):3616-21. doi: 10.1016/j.bmcl.2008.04.066. Epub 2008 May 1.

PMID:
18487044
[PubMed - indexed for MEDLINE]
2.

Hexahydro-pyrrolo- and hexahydro-1H-pyrido[1,2-b]pyridazin-2-ones as potent inhibitors of HCV NS5B polymerase.

Ruebsam F, Sun Z, Ayida BK, Webber SE, Zhou Y, Zhao Q, Kissinger CR, Showalter RE, Shah AM, Tsan M, Patel R, Lebrun LA, Kamran R, Sergeeva MV, Bartkowski DM, Nolan TG, Norris DA, Kirkovsky L.

Bioorg Med Chem Lett. 2008 Sep 15;18(18):5002-5. doi: 10.1016/j.bmcl.2008.08.017. Epub 2008 Aug 9.

PMID:
18722768
[PubMed - indexed for MEDLINE]
3.

4-(1,1-Dioxo-1,4-dihydro-1lambda6-benzo[1,4]thiazin-3-yl)-5-hydroxy-2H-pyridazin-3-ones as potent inhibitors of HCV NS5B polymerase.

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

Bioorg Med Chem Lett. 2008 Aug 15;18(16):4628-32. doi: 10.1016/j.bmcl.2008.07.014. Epub 2008 Jul 10.

PMID:
18662878
[PubMed - indexed for MEDLINE]
4.

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 3: Further optimization of the 2-, 6-, and 7'-substituents and initial pharmacokinetic assessments.

Li LS, Zhou Y, Murphy DE, Stankovic N, Zhao J, Dragovich PS, Bertolini T, Sun Z, Ayida B, Tran CV, Ruebsam F, Webber SE, Shah AM, Tsan M, Showalter RE, Patel R, Lebrun LA, Bartkowski DM, Nolan TG, Norris DA, Kamran R, Brooks J, Sergeeva MV, Kirkovsky L, Zhao Q, Kissinger CR.

Bioorg Med Chem Lett. 2008 Jun 1;18(11):3446-55. doi: 10.1016/j.bmcl.2008.02.072. Epub 2008 Mar 5.

PMID:
18457949
[PubMed - indexed for MEDLINE]
5.

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
[PubMed - indexed for MEDLINE]
6.

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 4. Optimization of DMPK properties.

Sergeeva MV, Zhou Y, Bartkowski DM, Nolan TG, Norris DA, Okamoto E, Kirkovsky L, Kamran R, Lebrun LA, Tsan M, Patel R, Shah AM, Lardy M, Gobbi A, Li LS, Zhao J, Bertolini T, Stankovic N, Sun Z, Murphy DE, Webber SE, Dragovich PS.

Bioorg Med Chem Lett. 2008 Jun 1;18(11):3421-6. doi: 10.1016/j.bmcl.2008.04.005. Epub 2008 Apr 4.

PMID:
18442904
[PubMed - indexed for MEDLINE]
7.

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
[PubMed - indexed for MEDLINE]
8.

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
[PubMed - indexed for MEDLINE]
9.

Identification of anthranilic acid derivatives as a novel class of allosteric inhibitors of hepatitis C NS5B polymerase.

Nittoli T, Curran K, Insaf S, DiGrandi M, Orlowski M, Chopra R, Agarwal A, Howe AY, Prashad A, Floyd MB, Johnson B, Sutherland A, Wheless K, Feld B, O'Connell J, Mansour TS, Bloom J.

J Med Chem. 2007 May 3;50(9):2108-16. Epub 2007 Apr 3. Erratum in: J Med Chem. 2007 Nov 29;50(24):6290.

PMID:
17402724
[PubMed - indexed for MEDLINE]
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
[PubMed - indexed for MEDLINE]
11.

Identification and biological evaluation of a series of 1H-benzo[de]isoquinoline-1,3(2H)-diones as hepatitis C virus NS5B polymerase inhibitors.

Ontoria JM, Rydberg EH, Di Marco S, Tomei L, Attenni B, Malancona S, Martin Hernando JI, Gennari N, Koch U, Narjes F, Rowley M, Summa V, Carroll SS, Olsen DB, De Francesco R, Altamura S, Migliaccio G, Carfì A.

J Med Chem. 2009 Aug 27;52(16):5217-27. doi: 10.1021/jm900517t.

PMID:
19877603
[PubMed - indexed for MEDLINE]
12.

Isothiazoles as active-site inhibitors of HCV NS5B polymerase.

Yan S, Appleby T, Gunic E, Shim JH, Tasu T, Kim H, Rong F, Chen H, Hamatake R, Wu JZ, Hong Z, Yao N.

Bioorg Med Chem Lett. 2007 Jan 1;17(1):28-33. Epub 2006 Oct 5.

PMID:
17049853
[PubMed - indexed for MEDLINE]
13.

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
[PubMed - indexed for MEDLINE]
14.

Discovery of proline sulfonamides as potent and selective hepatitis C virus NS5b polymerase inhibitors. Evidence for a new NS5b polymerase binding site.

Gopalsamy A, Chopra R, Lim K, Ciszewski G, Shi M, Curran KJ, Sukits SF, Svenson K, Bard J, Ellingboe JW, Agarwal A, Krishnamurthy G, Howe AY, Orlowski M, Feld B, O'Connell J, Mansour TS.

J Med Chem. 2006 Jun 1;49(11):3052-5.

PMID:
16722622
[PubMed - indexed for MEDLINE]
15.

Discovery of tricyclic 5,6-dihydro-1H-pyridin-2-ones as novel, potent, and orally bioavailable inhibitors of HCV NS5B polymerase.

Ruebsam F, Murphy DE, Tran CV, Li LS, Zhao J, Dragovich PS, McGuire HM, Xiang AX, Sun Z, Ayida BK, Blazel JK, Kim SH, Zhou Y, Han Q, Kissinger CR, Webber SE, Showalter RE, Shah AM, Tsan M, Patel RA, Thompson PA, Lebrun LA, Hou HJ, Kamran R, Sergeeva MV, Bartkowski DM, Nolan TG, Norris DA, Khandurina J, Brooks J, Okamoto E, Kirkovsky L.

Bioorg Med Chem Lett. 2009 Nov 15;19(22):6404-12. doi: 10.1016/j.bmcl.2009.09.045. Epub 2009 Sep 17.

PMID:
19818610
[PubMed - indexed for MEDLINE]
16.

Discovery of pyrano[3,4-b]indoles as potent and selective HCV NS5B polymerase inhibitors.

Gopalsamy A, Lim K, Ciszewski G, Park K, Ellingboe JW, Bloom J, Insaf S, Upeslacis J, Mansour TS, Krishnamurthy G, Damarla M, Pyatski Y, Ho D, Howe AY, Orlowski M, Feld B, O'Connell J.

J Med Chem. 2004 Dec 16;47(26):6603-8.

PMID:
15588095
[PubMed - indexed for MEDLINE]
17.

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
[PubMed - indexed for MEDLINE]
18.

1,5-Benzodiazepine inhibitors of HCV NS5B polymerase.

McGowan D, Nyanguile O, Cummings MD, Vendeville S, Vandyck K, Van den Broeck W, Boutton CW, De Bondt H, Quirynen L, Amssoms K, Bonfanti JF, Last S, Rombauts K, Tahri A, Hu L, Delouvroy F, Vermeiren K, Vandercruyssen G, Van der Helm L, Cleiren E, Mostmans W, Lory P, Pille G, Van Emelen K, Fanning G, Pauwels F, Lin TI, Simmen K, Raboisson P.

Bioorg Med Chem Lett. 2009 May 1;19(9):2492-6. doi: 10.1016/j.bmcl.2009.03.035. Epub 2009 Mar 14.

PMID:
19342234
[PubMed - indexed for MEDLINE]
19.

Structural basis for resistance of the genotype 2b hepatitis C virus NS5B polymerase to site A non-nucleoside inhibitors.

Rydberg EH, Cellucci A, Bartholomew L, Mattu M, Barbato G, Ludmerer SW, Graham DJ, Altamura S, Paonessa G, De Francesco R, Migliaccio G, CarfĂ­ A.

J Mol Biol. 2009 Jul 31;390(5):1048-59. doi: 10.1016/j.jmb.2009.06.012. Epub 2009 Jun 6.

PMID:
19505479
[PubMed - indexed for MEDLINE]
20.

Discovery of substituted N-phenylbenzenesulphonamides as a novel class of non-nucleoside hepatitis C virus polymerase inhibitors.

May MM, Brohm D, Harrenga A, Marquardt T, Riedl B, Kreuter J, Zimmermann H, Ruebsamen-Schaeff H, Urban A.

Antiviral Res. 2012 Aug;95(2):182-91. doi: 10.1016/j.antiviral.2012.04.008. Epub 2012 May 10.

PMID:
22580131
[PubMed - indexed for MEDLINE]

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