Results 201 to 210 of about 9,765 (234)

HCV NS5A replication complex inhibitors. Part 2: Investigation of stilbene prolinamides

Bioorganic & Medicinal Chemistry Letters, 2012
In a previous disclosure,(1) we reported the dimerization of an iminothiazolidinone to form 1, a contributor to the observed inhibition of HCV genotype 1b replicon activity. The dimer was isolated via bioassay-guided fractionation experiments and shown to be a potent inhibitor of genotype 1b HCV replication for which resistance mapped to the NS5A ...
Denis R, St Laurent, Makonen, Belema, Min, Gao, Jason, Goodrich, Ramesh, Kakarla, Jay O, Knipe, Julie A, Lemm, Mengping, Liu, Omar D, Lopez, Van N, Nguyen, Peter T, Nower, Donald, O'Boyle, Yuping, Qiu, Jeffrey L, Romine, Michael H, Serrano-Wu, Jin-Hua, Sun, Lourdes, Valera, Fukang, Yang, Xuejie, Yang, Nicholas A, Meanwell, Lawrence B, Snyder   +20 more
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[Research progress of HCV NS5A complex inhibitors].

Yao xue xue bao = Acta pharmaceutica Sinica, 2018
Direct acting antivirals against the hepatitis C virus (HCV) have been developed and the field has been under a rapid progress in recent years. Especially, HCV inhibitors targeting nonstructural 5A (NS5A) protein are attracting much attention due to the potent antiviral activity, fast viral clearance and broad antiviral spectrum.
Xin-bei, Jiang, Yan-ping, Li, Zhuo-rong, Li   +2 more
openaire   +1 more source

Discovery of ABT-267, a Pan-Genotypic Inhibitor of HCV NS5A

Journal of Medicinal Chemistry, 2014
We describe here N-phenylpyrrolidine-based inhibitors of HCV NS5A with excellent potency, metabolic stability, and pharmacokinetics. Compounds with 2S,5S stereochemistry at the pyrrolidine ring provided improved genotype 1 (GT1) potency compared to the 2R,5R analogues.
David A, DeGoey, John T, Randolph, Dachun, Liu, John, Pratt, Charles, Hutchins, Pamela, Donner, A Chris, Krueger, Mark, Matulenko, Sachin, Patel, Christopher E, Motter, Lissa, Nelson, Ryan, Keddy, Michael, Tufano, Daniel D, Caspi, Preethi, Krishnan, Neeta, Mistry, Gennadiy, Koev, Thomas J, Reisch, Rubina, Mondal, Tami, Pilot-Matias, Yi, Gao, David W A, Beno, Clarence J, Maring, Akhter, Molla, Emily, Dumas, Andrew, Campbell, Laura, Williams, Christine, Collins, Rolf, Wagner, Warren M, Kati   +29 more
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Discovery of pyrido[2,3-d]pyrimidine-based inhibitors of HCV NS5A

Bioorganic & Medicinal Chemistry Letters, 2013
Efforts to improve the genotype 1a potency and pharmacokinetics of earlier naphthyridine-based HCV NS5A inhibitors resulted in the discovery of a novel series of pyrido[2,3-d]pyrimidine compounds, which displayed potent inhibition of HCV genotypes 1a and 1b in the replicon assay.
David A, DeGoey, David A, Betebenner, David J, Grampovnik, Dachun, Liu, John K, Pratt, Michael D, Tufano, Wenping, He, Preethi, Krishnan, Tami J, Pilot-Matias, Kennan C, Marsh, Akhteruzzaman, Molla, Dale J, Kempf, Clarence J, Maring   +12 more
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Hepatitis C Virus NS5A Replication Complex Inhibitors: The Discovery of Daclatasvir

Journal of Medicinal Chemistry, 2014
The biphenyl derivatives 2 and 3 are prototypes of a novel class of NS5A replication complex inhibitors that demonstrate high inhibitory potency toward a panel of clinically relevant HCV strains encompassing genotypes 1-6. However, these compounds exhibit poor systemic exposure in rat pharmacokinetic studies after oral dosing.
Makonen, Belema, Van N, Nguyen, Carol, Bachand, Dan H, Deon, Jason T, Goodrich, Clint A, James, Rico, Lavoie, Omar D, Lopez, Alain, Martel, Jeffrey L, Romine, Edward H, Ruediger, Lawrence B, Snyder, Denis R, St Laurent, Fukang, Yang, Juliang, Zhu, Henry S, Wong, David R, Langley, Stephen P, Adams, Glenn H, Cantor, Anjaneya, Chimalakonda, Aberra, Fura, Benjamin M, Johnson, Jay O, Knipe, Dawn D, Parker, Kenneth S, Santone, Robert A, Fridell, Julie A, Lemm, Donald R, O'Boyle, Richard J, Colonno, Min, Gao, Nicholas A, Meanwell, Lawrence G, Hamann   +31 more
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Antiviral activity and resistance of HCV NS5A replication complex inhibitors

Current Opinion in Virology, 2013
Treatment of Hepatitis C Virus (HCV) infection is rapidly evolving with the introduction of direct acting antiviral agents (DAA). HCV NS5A replication complex inhibitors, exemplified by Daclatasvir (BMS-790052), represent a new class of DAA. The exceptional in vitro potency (EC50 values at pM to low nM range) and broad genotype coverage of NS5A ...
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Discovery and Development of Hepatitis C Virus NS5A Replication Complex Inhibitors

Journal of Medicinal Chemistry, 2014
Lead inhibitors that target the function of the hepatitis C virus (HCV) nonstructural 5A (NS5A) protein have been identified by phenotypic screening campaigns using HCV subgenomic replicons. The demonstration of antiviral activity in HCV-infected subjects by the HCV NS5A replication complex inhibitor (RCI) daclatasvir (1) spawned considerable interest ...
Makonen, Belema, Omar D, Lopez, John A, Bender, Jeffrey L, Romine, Denis R, St Laurent, David R, Langley, Julie A, Lemm, Donald R, O'Boyle, Jin-Hua, Sun, Chunfu, Wang, Robert A, Fridell, Nicholas A, Meanwell   +11 more
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Prevalence of NS5A resistance associated variants in NS5A inhibitor treatment failures and an effective treatment for NS5A-P32 deleted hepatitis C virus in humanized mice

Biochemical and Biophysical Research Communications, 2018
Patients with chronic hepatitis C virus (HCV) infection who have failed to respond to direct-acting antiviral (DAA) treatment often acquire drug resistance-associated variants (RAVs). The NS5A-P32 deletion (P32del) RAV confers potent resistance to NS5A inhibitors; therefore, patients who acquire this deletion are likely to fail to respond to DAA re ...
Yuji Teraoka, Takuro Uchida, Michio Imamura, Mitsutaka Osawa, Masataka Tsuge, Hiromi Abe-Chayama, C. Nelson Hayes, Grace Naswa Makokha, Hiroshi Aikata, Daiki Miki, Hidenori Ochi, Yuji Ishida, Chise Tateno, Kazuaki Chayama   +13 more
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The broadening scope of oral mucositis and oral ulcerative mucosal toxicities of anticancer therapies

Ca-A Cancer Journal for Clinicians, 2022
Sharon Elad, Noam Yarom, Yehuda Zadik
exaly  

NS5A inhibitors to treat hepatitis C virus infection

The Lancet Infectious Diseases, 2012
Tania M, Welzel, Stefan, Zeuzem
openaire   +2 more sources