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Items: 1 to 20 of 558

1.

HCV NS5B polymerase inhibitors 1: Synthesis and in vitro activity of 2-(1,1-dioxo-2H-[1,2,4]benzothiadiazin-3-yl)-1-hydroxynaphthalene derivatives.

Wang G, He Y, Sun J, Das D, Hu M, Huang J, Ruhrmund D, Hooi L, Misialek S, Ravi Rajagopalan PT, Stoycheva A, Buckman BO, Kossen K, Seiwert SD, Beigelman L.

Bioorg Med Chem Lett. 2009 Aug 1;19(15):4476-9. doi: 10.1016/j.bmcl.2009.05.063. Epub 2009 May 23.

PMID:
19502055
2.

HCV NS5B polymerase inhibitors 3: Synthesis and in vitro activity of 3-(1,1-dioxo-2H-[1,2,4]benzothiadiazin-3-yl)-4-hydroxy-2H-quinolizin-2-one derivatives.

Wang G, Zhang L, Wu X, Das D, Ruhrmund D, Hooi L, Misialek S, Ravi Rajagopalan PT, Buckman BO, Kossen K, Seiwert SD, Beigelman L.

Bioorg Med Chem Lett. 2009 Aug 1;19(15):4484-7. doi: 10.1016/j.bmcl.2009.05.021. Epub 2009 May 9.

PMID:
19497737
3.

HCV NS5B polymerase inhibitors 2: Synthesis and in vitro activity of (1,1-dioxo-2H-[1,2,4]benzothiadiazin-3-yl) azolo[1,5-a]pyridine and azolo[1,5-a]pyrimidine derivatives.

Wang G, Lei H, Wang X, Das D, Hong J, Mackinnon CH, Coulter TS, Montalbetti CA, Mears R, Gai X, Bailey SE, Ruhrmund D, Hooi L, Misialek S, Rajagopalan PT, Cheng RK, Barker JJ, Felicetti B, Schönfeld DL, Stoycheva A, Buckman BO, Kossen K, Seiwert SD, Beigelman L.

Bioorg Med Chem Lett. 2009 Aug 1;19(15):4480-3. doi: 10.1016/j.bmcl.2009.05.022. Epub 2009 May 9.

PMID:
19500983
4.

Synthesis and biological activity of heteroaryl 3-(1,1-dioxo-2H-(1,2,4)-benzothiadizin-3-yl)-4-hydroxy-2(1H)-quinolinone derivatives as hepatitis C virus NS5B polymerase inhibitors.

Tedesco R, Chai D, Darcy MG, Dhanak D, Fitch DM, Gates A, Johnston VK, Keenan RM, Lin-Goerke J, Sarisky RT, Shaw AN, Valko KL, Wiggall KJ, Zimmerman MN, Duffy KJ.

Bioorg Med Chem Lett. 2009 Aug 1;19(15):4354-8. doi: 10.1016/j.bmcl.2009.05.080. Epub 2009 May 27.

PMID:
19505821
5.

Substituted benzothiadizine inhibitors of Hepatitis C virus polymerase.

Shaw AN, Tedesco R, Bambal R, Chai D, Concha NO, Darcy MG, Dhanak D, Duffy KJ, Fitch DM, Gates A, Johnston VK, Keenan RM, Lin-Goerke J, Liu N, Sarisky RT, Wiggall KJ, Zimmerman MN.

Bioorg Med Chem Lett. 2009 Aug 1;19(15):4350-3. doi: 10.1016/j.bmcl.2009.05.091. Epub 2009 May 28.

PMID:
19515564
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.

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
8.

Hepatitis C NS5B polymerase inhibitors: 4,4-Dialkyl-1-hydroxy-3-oxo-3,4-dihydronaphthalene-3-yl benzothiadiazine derivatives.

Hutchinson DK, Rosenberg T, Klein LL, Bosse TD, Larson DP, He W, Jiang WW, Kati WM, Kohlbrenner WE, Liu Y, Masse SV, Middleton T, Molla A, Montgomery DA, Beno DW, Stewart KD, Stoll VS, Kempf DJ.

Bioorg Med Chem Lett. 2008 Jul 15;18(14):3887-90. doi: 10.1016/j.bmcl.2008.06.043. Epub 2008 Jun 18.

PMID:
18599294
9.

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
10.

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
11.

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
12.

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
13.

Phosphorous acid analogs of novel P2-P4 macrocycles as inhibitors of HCV-NS3 protease.

Pompei M, Francesco ME, Koch U, Liverton NJ, Summa V.

Bioorg Med Chem Lett. 2009 May 1;19(9):2574-8. doi: 10.1016/j.bmcl.2009.03.038. Epub 2009 Mar 17.

PMID:
19328685
14.

Inhibitors of HCV NS5B polymerase: synthesis and structure-activity relationships of N-1-heteroalkyl-4-hydroxyquinolon-3-yl-benzothiadiazines.

Pratt JK, Donner P, McDaniel KF, Maring CJ, Kati WM, Mo H, Middleton T, Liu Y, Ng T, Xie Q, Zhang R, Montgomery D, Molla A, Kempf DJ, Kohlbrenner W.

Bioorg Med Chem Lett. 2005 Mar 15;15(6):1577-82.

PMID:
15745800
15.

Inhibitors of HCV NS5B polymerase: synthesis and structure-activity relationships of N-alkyl-4-hydroxyquinolon-3-yl-benzothiadiazine sulfamides.

Krueger AC, Madigan DL, Jiang WW, Kati WM, Liu D, Liu Y, Maring CJ, Masse S, McDaniel KF, Middleton T, Mo H, Molla A, Montgomery D, Pratt JK, Rockway TW, Zhang R, Kempf DJ.

Bioorg Med Chem Lett. 2006 Jul 1;16(13):3367-70. Epub 2006 May 2.

PMID:
16650764
16.

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
17.

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
18.

Design and synthesis of indole, 2,3-dihydro-indole, and 3,4-dihydro-2H-quinoline-1-carbothioic acid amide derivatives as novel HCV inhibitors.

Kang IJ, Wang LW, Hsu SJ, Lee CC, Lee YC, Wu YS, Hsu TA, Yueh A, Chao YS, Chern JH.

Bioorg Med Chem Lett. 2009 Aug 1;19(15):4134-8. doi: 10.1016/j.bmcl.2009.06.009. Epub 2009 Jun 6.

PMID:
19539472
19.

3-(1,1-dioxo-2H-(1,2,4)-benzothiadiazin-3-yl)-4-hydroxy-2(1H)-quinolinones, potent inhibitors of hepatitis C virus RNA-dependent RNA polymerase.

Tedesco R, Shaw AN, Bambal R, Chai D, Concha NO, Darcy MG, Dhanak D, Fitch DM, Gates A, Gerhardt WG, Halegoua DL, Han C, Hofmann GA, Johnston VK, Kaura AC, Liu N, Keenan RM, Lin-Goerke J, Sarisky RT, Wiggall KJ, Zimmerman MN, Duffy KJ.

J Med Chem. 2006 Feb 9;49(3):971-83.

PMID:
16451063
20.

Studies on acyl pyrrolidine inhibitors of HCV RNA-dependent RNA polymerase to identify a molecule with replicon antiviral activity.

Burton G, Ku TW, Carr TJ, Kiesow T, Sarisky RT, Lin-Goerke J, Hofmann GA, Slater MJ, Haigh D, Dhanak D, Johnson VK, Parry NR, Thommes P.

Bioorg Med Chem Lett. 2007 Apr 1;17(7):1930-3. Epub 2007 Jan 19.

PMID:
17270443

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