Literature DB >> 23043370

(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.

Blake P Moore1, 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.   

Abstract

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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Year:  2012        PMID： 23043370      PMCID： PMC3506029          DOI： 10.1021/jm300612z

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  28 in total

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Authors:  Janet L Douglas; Marites L Panis; Edmund Ho; Kuei-Ying Lin; Steve H Krawczyk; Deborah M Grant; Ruby Cai; Swami Swaminathan; Tomas Cihlar
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2.  A BSL-4 high-throughput screen identifies sulfonamide inhibitors of Nipah virus.

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Journal:  J Med Chem       Date:  2014-12-04       Impact factor: 7.446

4.  Benzimidazole analogs inhibit respiratory syncytial virus G protein function.

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5.  5-((1H-imidazol-1-yl)methyl)quinolin-8-ol as potential antiviral SARS-CoV-2 candidate: Synthesis, crystal structure, Hirshfeld surface analysis, DFT and molecular docking studies.

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Review 6.  Synthetic and medicinal perspective of quinolines as antiviral agents.

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7.  A cell based high-throughput screening approach for the discovery of new inhibitors of respiratory syncytial virus.

Authors:  Dong-Hoon Chung; Blake P Moore; Daljit S Matharu; Jennifer E Golden; Clinton Maddox; Lynn Rasmussen; Melinda I Sosa; Subramaniam Ananthan; E Lucile White; Fuli Jia; Colleen B Jonsson; William E Severson
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  8 in total

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