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14 results on '"Goodrich, Jason T."'

2. HCV NS5A replication complex inhibitors. Part 3 : discovery of potent analogs with distinct core topologies

Author

Lopez, Omar D., Nguyen, Van N., St. Laurent, Denis R., Belema, Makonen, Serrano-Wu, Michael H., Goodrich, Jason T., Yang, Fukang, Qiu, Yuping, Ripka, Amy S., Nower, Peter T., Valera, Lourdes, Liu, Mengping, O’Boyle, Donald R., II, Sun, Jin-Hua, Fridell, Robert A., Lemm, Julie A., Gao, Min, Good, Andrew C., Meanwell, Nicholas A., and Snyder, Lawrence B.

Published
2013
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3. Hepatitis C Virus NS5A Replication Complex Inhibitors: The Discovery of Daclatasvir

Author

Belema, Makonen, primary, Nguyen, Van N., additional, Bachand, Carol, additional, Deon, Dan H., additional, Goodrich, Jason T., additional, James, Clint A., additional, Lavoie, Rico, additional, Lopez, Omar D., additional, Martel, Alain, additional, Romine, Jeffrey L., additional, Ruediger, Edward H., additional, Snyder, Lawrence B., additional, St. Laurent, Denis R., additional, Yang, Fukang, additional, Zhu, Juliang, additional, Wong, Henry S., additional, Langley, David R., additional, Adams, Stephen P., additional, Cantor, Glenn H., additional, Chimalakonda, Anjaneya, additional, Fura, Aberra, additional, Johnson, Benjamin M., additional, Knipe, Jay O., additional, Parker, Dawn D., additional, Santone, Kenneth S., additional, Fridell, Robert A., additional, Lemm, Julie A., additional, O’Boyle, Donald R., additional, Colonno, Richard J., additional, Gao, Min, additional, Meanwell, Nicholas A., additional, and Hamann, Lawrence G., additional

Published
2014
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4. Hepatitis C Virus NS5A Replication Complex Inhibitors. Part 6: Discovery of a Novel and Highly Potent Biarylimidazole Chemotype with Inhibitory Activity Toward Genotypes 1a and 1b Replicons

Author

Belema, Makonen, primary, Nguyen, Van N., additional, Romine, Jeffrey L., additional, St. Laurent, Denis R., additional, Lopez, Omar D., additional, Goodrich, Jason T., additional, Nower, Peter T., additional, O’Boyle, Donald R., additional, Lemm, Julie A., additional, Fridell, Robert A., additional, Gao, Min, additional, Fang, Hua, additional, Krause, Rudolph G., additional, Wang, Ying-Kai, additional, Oliver, A. Jayne, additional, Good, Andrew C., additional, Knipe, Jay O., additional, Meanwell, Nicholas A., additional, and Snyder, Lawrence B., additional

Published
2014
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5. HCV NS5A Replication Complex Inhibitors. Part 4.1 Optimization for Genotype 1a Replicon Inhibitory Activity

Author

St. Laurent, Denis R., primary, Serrano-Wu, Michael H., additional, Belema, Makonen, additional, Ding, Min, additional, Fang, Hua, additional, Gao, Min, additional, Goodrich, Jason T., additional, Krause, Rudolph G., additional, Lemm, Julie A., additional, Liu, Mengping, additional, Lopez, Omar D., additional, Nguyen, Van N., additional, Nower, Peter T., additional, O’Boyle, Donald R., additional, Pearce, Bradley C., additional, Romine, Jeffrey L., additional, Valera, Lourdes, additional, Sun, Jin-Hua, additional, Wang, Ying-Kai, additional, Yang, Fukang, additional, Yang, Xuejie, additional, Meanwell, Nicholas A., additional, and Snyder, Lawrence B., additional

Published
2013
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11. Hepatitis C Virus NS5A ReplicationComplex Inhibitors.Part 6: Discovery of a Novel and Highly Potent Biarylimidazole Chemotypewith Inhibitory Activity Toward Genotypes 1a and 1b Replicons.

Author

Belema, Makonen, Nguyen, Van N., Romine, Jeffrey L., St. Laurent, Denis R., Lopez, Omar D., Goodrich, Jason T., Nower, Peter T., O’Boyle, Donald R., Lemm, Julie A., Fridell, Robert A., Gao, Min, Fang, Hua, Krause, Rudolph G., Wang, Ying-Kai, Oliver, A. Jayne, Good, Andrew C., Knipe, Jay O., Meanwell, Nicholas A., and Snyder, Lawrence B.

Published
2014
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12. HCV NS5AReplication Complex Inhibitors. Part 4.1 Optimization for Genotype 1a Replicon InhibitoryActivity.

Author

St. Laurent, Denis R., Serrano-Wu, Michael H., Belema, Makonen, Ding, Min, Fang, Hua, Gao, Min, Goodrich, Jason T., Krause, Rudolph G., Lemm, Julie A., Liu, Mengping, Lopez, Omar D., Nguyen, Van N., Nower, Peter T., O’Boyle, Donald R., Pearce, Bradley C., Romine, Jeffrey L., Valera, Lourdes, Sun, Jin-Hua, Wang, Ying-Kai, and Yang, Fukang

Published
2014
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13. HCV NS5A replication complex inhibitors. Part 31: discovery of potent analogs with distinct core topologies

Author

Lopez, Omar D., Nguyen, Van N., St. Laurent, Denis R., Belema, Makonen, Serrano-Wu, Michael H., Goodrich, Jason T., Yang, Fukang, Qiu, Yuping, Ripka, Amy S., Nower, Peter T., Valera, Lourdes, Liu, Mengping, O’Boyle, Donald R., Sun, Jin-Hua, Fridell, Robert A., Lemm, Julie A., Gao, Min, Good, Andrew C., Meanwell, Nicholas A., and Snyder, Lawrence B.

Subjects
*HEPATITIS C virus, *VIRAL replication, *AMIDES, *REPLICONS, *STRUCTURE-activity relationships, *TOPOLOGY
Abstract

Abstract: In a recent disclosure,1 we described the discovery of dimeric, prolinamide-based NS5A replication complex inhibitors exhibiting excellent potency towards an HCV genotype 1b replicon. That disclosure dealt with the SAR exploration of the peripheral region of our lead chemotype, and herein is described the SAR uncovered from a complementary effort that focused on the central core region. From this effort, the contribution of the core region to the overall topology of the pharmacophore, primarily vector orientation and planarity, was determined, with a set of analogs exhibiting <10nM EC50 in a genotype 1b replicon assay. [Copyright &y& Elsevier]

Published
2013
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14. HCV NS5A replication complex inhibitors. Part 4. Optimization for genotype 1a replicon inhibitory activity.

Author

St Laurent DR, Serrano-Wu MH, Belema M, Ding M, Fang H, Gao M, Goodrich JT, Krause RG, Lemm JA, Liu M, Lopez OD, Nguyen VN, Nower PT, O'Boyle DR 2nd, Pearce BC, Romine JL, Valera L, Sun JH, Wang YK, Yang F, Yang X, Meanwell NA, and Snyder LB

Subjects
Antiviral Agents chemistry, Hepacivirus genetics, Hepacivirus physiology, Magnetic Resonance Spectroscopy, Models, Molecular, Protease Inhibitors chemistry, Spectrometry, Mass, Electrospray Ionization, Antiviral Agents pharmacology, Genotype, Hepacivirus drug effects, Protease Inhibitors pharmacology, RNA-Dependent RNA Polymerase antagonists & inhibitors, Replicon drug effects, Viral Nonstructural Proteins antagonists & inhibitors, Virus Replication drug effects
Abstract

A series of symmetrical E-stilbene prolinamides that originated from the library-synthesized lead 3 was studied with respect to HCV genotype 1a (G-1a) and genotype 1b (G-1b) replicon inhibition and selectivity against BVDV and cytotoxicity. SAR emerging from an examination of the prolinamide cap region revealed 11 to be a selective HCV NS5A inhibitor exhibiting submicromolar potency against both G-1a and G-1b replicons. Additional structural refinements resulted in the identification of 30 as a potent, dual G-1a/1b HCV NS5A inhibitor.

Published
2014
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