Literature DB >> 25229881

Identification, synthesis, and evaluation of new neuraminidase inhibitors.

Vathan Kumar1, Chih-Kang Chang, Kian-Pin Tan, Young-Sik Jung, Shih-Hsun Chen, Yih-Shyun E Cheng, Po-Huang Liang.   

Abstract

High-throughput screening was performed on ∼6800 compounds to identify KR-72039 as an inhibitor of H1N1 and H5N1 neuraminidases (NAs). Structure-activity relationship studies led to 3e, which inhibited H5N1 NA with an IC50 of 2.8 μM and blocked viral replication. Docking analysis shows that compounds bind to loop-430 around the NA active site. Compound 3l additionally inhibited H7N9 NA, making it a dual inhibitor of N1- and N2-type NAs.

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Year:  2014        PMID： 25229881     DOI： 10.1021/ol502410x

Source DB:  PubMed          Journal:  Org Lett        ISSN： 1523-7052            Impact factor:   6.005


  6 in total

1.  Inhibition of the FAD containing ER oxidoreductin 1 (Ero1) protein by EN-460 as a strategy for treatment of multiple myeloma.

Authors:  Karen E Hayes; Paratchata Batsomboon; Wei-Chih Chen; Brennan D Johnson; Andreas Becker; Steven Eschrich; Yan Yang; Aaron R Robart; Gregory B Dudley; Werner J Geldenhuys; Lori A Hazlehurst
Journal:  Bioorg Med Chem       Date:  2019-02-10       Impact factor: 3.641

2.  Discovery of Novel Neuraminidase Inhibitors by Structure-Based Virtual Screening, Structural Optimization, and Bioassay.

Authors:  Rao Yu; Li Ping Cheng; Meng Li; Wan Pang
Journal:  ACS Med Chem Lett       Date:  2019-11-25       Impact factor: 4.345

3.  Design and Structure-Guided Development of Novel Inhibitors of the Xeroderma Pigmentosum Group A (XPA) Protein-DNA Interaction.

Authors:  Navnath S Gavande; Pamela VanderVere-Carozza; Akaash K Mishra; Tyler L Vernon; Katherine S Pawelczak; John J Turchi
Journal:  J Med Chem       Date:  2017-09-21       Impact factor: 7.446

4.  Identification, synthesis and evaluation of SARS-CoV and MERS-CoV 3C-like protease inhibitors.

Authors:  Vathan Kumar; Kian-Pin Tan; Ying-Ming Wang; Sheng-Wei Lin; Po-Huang Liang
Journal:  Bioorg Med Chem       Date:  2016-05-12       Impact factor: 3.641

Review 5.  Synthetic and computational efforts towards the development of peptidomimetics and small-molecule SARS-CoV 3CLpro inhibitors.

Authors:  Abhik Paul; Arnab Sarkar; Sanjukta Saha; Avik Maji; Pritha Janah; Tapan Kumar Maity
Journal:  Bioorg Med Chem       Date:  2021-07-03       Impact factor: 3.641

Review 6.  The recent outbreaks of human coronaviruses: A medicinal chemistry perspective.

Authors:  Thanigaimalai Pillaiyar; Lukas L Wendt; Manoj Manickam; Maheswaran Easwaran
Journal:  Med Res Rev       Date:  2020-08-27       Impact factor: 12.388
  6 in total

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