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Items: 1 to 20 of 100

1.

Discovery of ITX 4520: a highly potent orally bioavailable hepatitis C virus entry inhibitor.

Mittapalli GK, Zhao F, Jackson A, Gao H, Lee H, Chow S, Kaur MP, Nguyen N, Zamboni R, McKelvy J, Wong-Staal F, Macdonald JE.

Bioorg Med Chem Lett. 2012 Aug 1;22(15):4955-61. doi: 10.1016/j.bmcl.2012.06.038. Epub 2012 Jun 19.

PMID:
22784640
2.

Discovery of highly potent small molecule Hepatitis C Virus entry inhibitors.

Mittapalli GK, Jackson A, Zhao F, Lee H, Chow S, McKelvy J, Wong-Staal F, Macdonald JE.

Bioorg Med Chem Lett. 2011 Nov 15;21(22):6852-5. doi: 10.1016/j.bmcl.2011.09.019. Epub 2011 Sep 16.

PMID:
21978675
3.

Allosteric inhibitors of hepatitis C polymerase: discovery of potent and orally bioavailable carbon-linked dihydropyrones.

Li H, Linton A, Tatlock J, Gonzalez J, Borchardt A, Abreo M, Jewell T, Patel L, Drowns M, Ludlum S, Goble M, Yang M, Blazel J, Rahavendran R, Skor H, Shi S, Lewis C, Fuhrman S.

J Med Chem. 2007 Aug 23;50(17):3969-72. Epub 2007 Jul 21.

PMID:
17658778
4.

Discovery and preclinical evaluation of potent, orally bioavailable, metabolically stable cyclopropylindolobenzazepine acylsulfonamides as thumb site 1 inhibitors of the hepatitis c virus NS5B RNA-dependent, RNA polymerase.

Hewawasam P, Tu Y, Gao M, Hanumegowda U, Knipe J, Lemm JA, Parker DD, Rigat KL, Roberts SB, Meanwell NA, Kadow JF.

Bioorg Med Chem Lett. 2016 Feb 1;26(3):936-40. doi: 10.1016/j.bmcl.2015.12.058. Epub 2015 Dec 19.

PMID:
26747393
5.

Synthesis and SAR of geminal substitutions at the C5' carbosugar position of pyrimidine-derived HCV inhibitors.

Verma VA, Rossman R, Bennett F, Chen L, Gavalas S, Girijavallabhan V, Huang Y, Kim SH, Kosinski A, Pinto P, Rizvi R, Shankar B, Tong L, Velazquez F, Venkatraman S, Kozlowski J, MacCoss M, Kwong CD, Bansal N, Kezar HS 3rd, Reynolds RC, Maddry JA, Ananthan S, Secrist JA 3rd, Li C, Chase R, Curry S, Huang HC, Tong X, Njoroge FG, Arasappan A.

Bioorg Med Chem Lett. 2012 Nov 15;22(22):6967-73. doi: 10.1016/j.bmcl.2012.08.111. Epub 2012 Sep 7.

PMID:
23036957
6.

Structure-activity relationship (SAR) optimization of 6-(indol-2-yl)pyridine-3-sulfonamides: identification of potent, selective, and orally bioavailable small molecules targeting hepatitis C (HCV) NS4B.

Zhang N, Zhang X, Zhu J, Turpoff A, Chen G, Morrill C, Huang S, Lennox W, Kakarla R, Liu R, Li C, Ren H, Almstead N, Venkatraman S, Njoroge FG, Gu Z, Clausen V, Graci J, Jung SP, Zheng Y, Colacino JM, Lahser F, Sheedy J, Mollin A, Weetall M, Nomeir A, Karp GM.

J Med Chem. 2014 Mar 13;57(5):2121-35. doi: 10.1021/jm401621g. Epub 2013 Dec 4.

PMID:
24266880
7.

Discovery of (7R)-14-cyclohexyl-7-{[2-(dimethylamino)ethyl](methyl) amino}-7,8-dihydro-6H-indolo[1,2-e][1,5]benzoxazocine-11-carboxylic acid (MK-3281), a potent and orally bioavailable finger-loop inhibitor of the hepatitis C virus NS5B polymerase.

Narjes F, Crescenzi B, Ferrara M, Habermann J, Colarusso S, Ferreira Mdel R, Stansfield I, Mackay AC, Conte I, Ercolani C, Zaramella S, Palumbi MC, Meuleman P, Leroux-Roels G, Giuliano C, Fiore F, Di Marco S, Baiocco P, Koch U, Migliaccio G, Altamura S, Laufer R, De Francesco R, Rowley M.

J Med Chem. 2011 Jan 13;54(1):289-301. doi: 10.1021/jm1013105. Epub 2010 Dec 8.

PMID:
21141896
8.

Discovery of (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), a selective, potent, orally bioavailable hepatitis C virus NS3 protease inhibitor: a potential therapeutic agent for the treatment of hepatitis C infection.

Venkatraman S, Bogen SL, Arasappan A, Bennett F, Chen K, Jao E, Liu YT, Lovey R, Hendrata S, Huang Y, Pan W, Parekh T, Pinto P, Popov V, Pike R, Ruan S, Santhanam B, Vibulbhan B, Wu W, Yang W, Kong J, Liang X, Wong J, Liu R, Butkiewicz N, Chase R, Hart A, Agrawal S, Ingravallo P, Pichardo J, Kong R, Baroudy B, Malcolm B, Guo Z, Prongay A, Madison V, Broske L, Cui X, Cheng KC, Hsieh Y, Brisson JM, Prelusky D, Korfmacher W, White R, Bogdanowich-Knipp S, Pavlovsky A, Bradley P, Saksena AK, Ganguly A, Piwinski J, Girijavallabhan V, Njoroge FG.

J Med Chem. 2006 Oct 5;49(20):6074-86.

PMID:
17004721
9.

Discovery and optimization of a novel series of N-arylamide oxadiazoles as potent, highly selective and orally bioavailable cannabinoid receptor 2 (CB2) agonists.

Cheng Y, Albrecht BK, Brown J, Buchanan JL, Buckner WH, DiMauro EF, Emkey R, Fremeau RT Jr, Harmange JC, Hoffman BJ, Huang L, Huang M, Lee JH, Lin FF, Martin MW, Nguyen HQ, Patel VF, Tomlinson SA, White RD, Xia X, Hitchcock SA.

J Med Chem. 2008 Aug 28;51(16):5019-34. doi: 10.1021/jm800463f. Epub 2008 Aug 5.

PMID:
18680277
10.

Discovery of an orally bioavailable alkyl oxadiazole beta3 adrenergic receptor agonist.

Feng DD, Biftu T, Candelore MR, Cascieri MA, Colwell LF Jr, Deng L, Feeney WP, Forrest MJ, Hom GJ, MacIntyre DE, Miller RR, Stearns RA, Strader CD, Tota L, Wyvratt MJ, Fisher MH, Weber AE.

Bioorg Med Chem Lett. 2000 Jul 3;10(13):1427-9.

PMID:
10888324
11.

Structure-activity relationship of heterobase-modified 2'-C-methyl ribonucleosides as inhibitors of hepatitis C virus RNA replication.

Eldrup AB, Prhavc M, Brooks J, Bhat B, Prakash TP, Song Q, Bera S, Bhat N, Dande P, Cook PD, Bennett CF, Carroll SS, Ball RG, Bosserman M, Burlein C, Colwell LF, Fay JF, Flores OA, Getty K, LaFemina RL, Leone J, MacCoss M, McMasters DR, Tomassini JE, Von Langen D, Wolanski B, Olsen DB.

J Med Chem. 2004 Oct 7;47(21):5284-97.

PMID:
15456273
12.

Activity of a potent hepatitis C virus polymerase inhibitor in the chimpanzee model.

Chen CM, He Y, Lu L, Lim HB, Tripathi RL, Middleton T, Hernandez LE, Beno DW, Long MA, Kati WM, Bosse TD, Larson DP, Wagner R, Lanford RE, Kohlbrenner WE, Kempf DJ, Pilot-Matias TJ, Molla A.

Antimicrob Agents Chemother. 2007 Dec;51(12):4290-6. Epub 2007 Oct 1.

13.

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
14.

Structure-activity relationship (SAR) development and discovery of potent indole-based inhibitors of the hepatitis C virus (HCV) NS5B polymerase.

Chen KX, Vibulbhan B, Yang W, Sannigrahi M, Velazquez F, Chan TY, Venkatraman S, Anilkumar GN, Zeng Q, Bennet F, Jiang Y, Lesburg CA, Duca J, Pinto P, Gavalas S, Huang Y, Wu W, Selyutin O, Agrawal S, Feld B, Huang HC, Li C, Cheng KC, Shih NY, Kozlowski JA, Rosenblum SB, Njoroge FG.

J Med Chem. 2012 Jan 26;55(2):754-65. doi: 10.1021/jm201258k. Epub 2012 Jan 6.

PMID:
22148957
15.

Potent bisimidazole-based HCV NS5A inhibitors bearing annulated tricyclic motifs.

Zhong M, Peng E, Huang N, Huang Q, Huq A, Lau M, Colonno R, Li L.

Bioorg Med Chem Lett. 2014 Dec 15;24(24):5738-42. doi: 10.1016/j.bmcl.2014.10.056. Epub 2014 Oct 22.

PMID:
25453811
16.

Structure-activity study on a novel series of macrocyclic inhibitors of the hepatitis C virus NS3 protease leading to the discovery of BILN 2061.

Llinàs-Brunet M, Bailey MD, Bolger G, Brochu C, Faucher AM, Ferland JM, Garneau M, Ghiro E, Gorys V, Grand-Maître C, Halmos T, Lapeyre-Paquette N, Liard F, Poirier M, Rhéaume M, Tsantrizos YS, Lamarre D.

J Med Chem. 2004 Mar 25;47(7):1605-8.

PMID:
15027850
17.

Second-generation highly potent and selective inhibitors of the hepatitis C virus NS3 serine protease.

Chen KX, Nair L, Vibulbhan B, Yang W, Arasappan A, Bogen SL, Venkatraman S, Bennett F, Pan W, Blackman ML, Padilla AI, Prongay A, Cheng KC, Tong X, Shih NY, Njoroge FG.

J Med Chem. 2009 Mar 12;52(5):1370-9. doi: 10.1021/jm801238q.

PMID:
19196021
18.

The discovery of potent nonstructural protein 5A (NS5A) inhibitors with a unique resistance profile-Part 1.

Tran TD, Wakenhut F, Pickford C, Shaw S, Westby M, Smith-Burchnell C, Watson L, Paradowski M, Milbank J, Brimage RA, Halstead R, Glen R, Wilson CP, Adam F, Hay D, Chiva JY, Nichols C, Blakemore DC, Gardner I, Dayal S, Pike A, Webster R, Pryde DC.

ChemMedChem. 2014 Jul;9(7):1378-86. doi: 10.1002/cmdc.201400045. Epub 2014 Apr 11.

PMID:
24729513
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.

Discovery of novel phosphonate derivatives as hepatitis C virus NS3 protease inhibitors.

Sheng XC, Pyun HJ, Chaudhary K, Wang J, Doerffler E, Fleury M, McMurtrie D, Chen X, Delaney WE 4th, Kim CU.

Bioorg Med Chem Lett. 2009 Jul 1;19(13):3453-7. doi: 10.1016/j.bmcl.2009.05.023. Epub 2009 May 9.

PMID:
19477126

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