| (S)-N-(2,5-Dimethylphenyl)-1-(quinoline-8-ylsulfonyl)pyrrolidine-2-carboxamide as a small molecule inhibitor probe for the study of respiratory syncytial virus infection. | |
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MedLine Citation:
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PMID: 23043370 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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A high-throughput, cell-based screen was used to identify chemotypes as inhibitors for human respiratory syncytial virus (hRSV). Optimization of a sulfonylpyrrolidine scaffold resulted in compound 5o that inhibited a virus-induced cytopathic effect in the entry stage of infection (EC₅₀ = 2.3 ± 0.8 μM) with marginal cytotoxicity (CC₅₀ = 30.9 ± 1.1 μM) and reduced viral titer by 100-fold. Compared to ribavirin, sulfonylpyrrolidine 5o demonstrated an improved in vitro potency and selectivity index. |
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Authors:
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Blake P Moore; Dong Hoon Chung; Daljit S Matharu; Jennifer E Golden; Clinton Maddox; Lynn Rasmussen; James W Noah; Melinda I Sosa; Subramaniam Ananthan; Nichole A Tower; E Lucile White; Fuli Jia; Thomas E Prisinzano; Jeffrey Aubé; Colleen B Jonsson; William E Severson |
Publication Detail:
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Type: Journal Article; Research Support, N.I.H., Extramural Date: 2012-10-16 |
Journal Detail:
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Title: Journal of medicinal chemistry Volume: 55 ISSN: 1520-4804 ISO Abbreviation: J. Med. Chem. Publication Date: 2012 Oct |
Date Detail:
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Created Date: 2012-10-25 Completed Date: 2013-02-05 Revised Date: 2013-04-16 |
Medline Journal Info:
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Nlm Unique ID: 9716531 Medline TA: J Med Chem Country: United States |
Other Details:
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Languages: eng Pagination: 8582-7 Citation Subset: IM |
Affiliation:
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Southern Research Specialized Biocontainment Screening Center, Southern Research Institute, Birmingham, Alabama 35205, USA. |
Export Citation:
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| MeSH Terms | |
Descriptor/Qualifier:
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Antiviral Agents
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chemical synthesis*,
chemistry,
pharmacology Cell Line, Tumor Cell Survival / drug effects Cytopathogenic Effect, Viral / drug effects High-Throughput Screening Assays Humans Pyrrolidines / chemical synthesis*, chemistry, pharmacology Quinolines / chemical synthesis*, chemistry, pharmacology Respiratory Syncytial Viruses / drug effects*, physiology Ribavirin / pharmacology Stereoisomerism Structure-Activity Relationship Sulfonamides / chemical synthesis*, chemistry, pharmacology Sulfones / chemical synthesis*, chemistry, pharmacology Viral Load / drug effects Virus Internalization / drug effects Virus Replication / drug effects |
| Grant Support | |
ID/Acronym/Agency:
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1 R03 MH082403-01A1/MH/NIMH NIH HHS; U54 HG005034-01/HG/NHGRI NIH HHS; U54HG005031/HG/NHGRI NIH HHS |
| Chemical | |
Reg. No./Substance:
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0/Antiviral Agents; 0/N-(2,5-dimethylphenyl)-1-(quinolin-8-ylsulfonyl)pyrrolidine-2-carboxamide; 0/Pyrrolidines; 0/Quinolines; 0/Sulfonamides; 0/Sulfones; 36791-04-5/Ribavirin |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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