ArticleACS medicinal chemistry letters2011
Inhibitors of HCV NS5A: From Iminothiazolidinones to Symmetrical Stilbenes.
Article in ACS medicinal chemistry letters, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.
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Who cites it
11 citing papers in PubMed.
- Recent Applications of Hydantoins in Drug Discovery: Updates (2019~Present).Molecules (Basel, Switzerland) · 2026Review
- Synthesis, crystal structure and Hirshfeld surface analysis of 2-[(4-hy-droxy-phen-yl)amino]-5,5-diphenyl-1Acta crystallographica. Section E, Crystallographic communications · 2024Article
- Progress, evolving therapeutic/diagnostic approaches, and challenges in the management of hepatitis C virus infections.Archives of virology · 2022Review
- The Compound SBI-0090799 Inhibits Zika Virus Infection by BlockingJournal of virology · 2021Article
- Saturated Five-Membered Thiazolidines and Their Derivatives: From Synthesis to Biological Applications.Topics in current chemistry (Cham) · 2020Review
- Article
- The crystal structure of NS5A domain 1 from genotype 1a reveals new clues to the mechanism of action for dimeric HCV inhibitors.Protein science : a publication of the Protein Society · 2014Article
- Potent Hepatitis C Virus NS5A Inhibitors Containing a Benzidine Core.ACS medicinal chemistry letters · 2014Article
- TARGETING THE NS5A PROTEIN OF HCV: AN EMERGING OPTION.Drugs of the future · 2011Article
- Discovery of potent hepatitis C virus NS5A inhibitors with dimeric structures.Antimicrobial agents and chemotherapy · 2011Article
- Synthesis and antiviral evaluation of 9-(S)-[3-alkoxy-2-(phosphonomethoxy)propyl]nucleoside alkoxyalkyl esters: inhibitors of hepatitis C virus and HIV-1 replication.Bioorganic & medicinal chemistry · 2011Article
Corrections and comments
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Authors and funding
15 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The iminothiazolidinone BMS-858 (2) was identified as a specific inhibitor of HCV replication in a genotype 1b replicon assay via a high-throughput screening campaign. A more potent analogue, BMS-824 (18), was used in resistance mapping studies, which revealed that inhibitory activity was related to disrupting the function of the HCV nonstructural protein 5A. Despite the development of coherent and interpretable SAR, it was subsequently discovered that in DMSO 18 underwent an oxidation and structural rearrangement to afford the thiohydantoin 47, a compound with reduced HCV inhibitory activity. However, HPLC bioassay fractionation studies performed after incubation of 18 in assay media led to the identification of fractions containing a dimeric species 48 that exhibited potent antiviral activity. Excision of the key elements hypothesized to be responsible for antiviral activity based on SAR observations reduced 48 to a simplified, symmetrical, pharmacophore realized most effectively with the stilbene 55, a compound that demonstrated potent inhibition of HCV in a genotype 1b replicon with an EC50 = 86 pM.
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