Literature DB >> 24900814

Potent Hepatitis C Virus NS5A Inhibitors Containing a Benzidine Core.

Il Hak Bae1, Jin Kyu Choi1, Chieyeon Chough1, Sun Ju Keum2, Heesun Kim2, Sung Key Jang2, B Moon Kim1.   

Abstract

Here we report the discovery of a series of potent hepatitis C virus (HCV) NS5A inhibitors based on the benzidine prolinamide backbone. Taking a simple synthetic route, we developed a novel inhibitor structure, which allows easy modification, and through optimization of the capping group, we identified compound 6 with highly potent anti-HCV activity. Compound 6 is nontoxic and is anticipated to be an effective HCV drug candidate.

Entities:  

Keywords:  HCV; NS5A inhibitor; antiviral agent; benzidine; structure−activity relationship

Year:  2013        PMID： 24900814      PMCID： PMC4027583          DOI： 10.1021/ml4003293

Source DB:  PubMed          Journal:  ACS Med Chem Lett        ISSN： 1948-5875            Impact factor:   4.345


  37 in total

1.  Ribonucleoside analogue that blocks replication of bovine viral diarrhea and hepatitis C viruses in culture.

Authors:  Lieven J Stuyver; Tony Whitaker; Tamara R McBrayer; Brenda I Hernandez-Santiago; Stefania Lostia; Phillip M Tharnish; Mangala Ramesh; Chung K Chu; Robert Jordan; Junxing Shi; Suguna Rachakonda; Kyoichi A Watanabe; Michael J Otto; Raymond F Schinazi
Journal:  Antimicrob Agents Chemother       Date:  2003-01       Impact factor: 5.191

2.  Prediction of hERG K+ blocking potency: application of structural knowledge.

Authors:  A O Aptula; M T D Cronin
Journal:  SAR QSAR Environ Res       Date:  2004 Oct-Dec       Impact factor: 3.000

Review 3.  Ribavirin for chronic hepatitis C: and the mystery goes on.

Authors:  Stefano Brillanti; Giuseppe Mazzella; Enrico Roda
Journal:  Dig Liver Dis       Date:  2010-11-18       Impact factor: 4.088

Review 4.  Assembly of infectious hepatitis C virus particles.

Authors:  Ralf Bartenschlager; Francois Penin; Volker Lohmann; Patrice André
Journal:  Trends Microbiol       Date:  2010-12-14       Impact factor: 17.079

5.  Contribution of complement system on destabilization of liposomes composed of hydrogenated egg phosphatidylcholine in rat fresh plasma.

Authors:  K Funato; R Yoda; H Kiwada
Journal:  Biochim Biophys Acta       Date:  1992-01-31

6.  Development of the predictor HERG fluorescence polarization assay using a membrane protein enrichment approach.

Authors:  David R Piper; Steve R Duff; Hildegard C Eliason; W Jack Frazee; Elizabeth A Frey; Maya Fuerstenau-Sharp; Christine Jachec; Bryan D Marks; Brian A Pollok; Mohammed Saleh Shekhani; David V Thompson; Pam Whitney; Kurt W Vogel; Stephen D Hess
Journal:  Assay Drug Dev Technol       Date:  2008-04       Impact factor: 1.738

7.  Synthesis and biological evaluation of new potent and selective HCV NS5A inhibitors.

Authors:  Junxing Shi; Longhu Zhou; Franck Amblard; Drew R Bobeck; Hongwang Zhang; Peng Liu; Lavanya Bondada; Tamara R McBrayer; Phillip M Tharnish; Tony Whitaker; Steven J Coats; Raymond F Schinazi
Journal:  Bioorg Med Chem Lett       Date:  2012-03-29       Impact factor: 2.823

8.  Correlation between NS5A dimerization and hepatitis C virus replication.

Authors:  Precious J Lim; Udayan Chatterji; Daniel Cordek; Suresh D Sharma; Jose A Garcia-Rivera; Craig E Cameron; Kai Lin; Paul Targett-Adams; Philippe A Gallay
Journal:  J Biol Chem       Date:  2012-07-16       Impact factor: 5.157

9.  Structure of the zinc-binding domain of an essential component of the hepatitis C virus replicase.

Authors:  Timothy L Tellinghuisen; Joseph Marcotrigiano; Charles M Rice
Journal:  Nature       Date:  2005-05-19       Impact factor: 49.962

10.  HCV NS5A replication complex inhibitors. Part 3: discovery of potent analogs with distinct core topologies.

Authors:  Omar D Lopez; Van N Nguyen; Denis R St Laurent; Makonen Belema; Michael H Serrano-Wu; Jason T Goodrich; Fukang Yang; Yuping Qiu; Amy S Ripka; Peter T Nower; Lourdes Valera; Mengping Liu; Donald R O'Boyle; Jin-Hua Sun; Robert A Fridell; Julie A Lemm; Min Gao; Andrew C Good; Nicholas A Meanwell; Lawrence B Snyder
Journal:  Bioorg Med Chem Lett       Date:  2012-12-03       Impact factor: 2.823
View more
  5 in total

1.  Design and Synthesis of Novel Bis-Imidazolyl Phenyl Butadiyne Derivatives as HCV NS5A Inhibitors.

Authors:  Jehad Hamdy; Nouran Emadeldin; Mostafa M Hamed; Efseveia Frakolaki; Sotirios Katsamakas; Niki Vassilaki; Grigoris Zoidis; Anna K H Hirsch; Mohammad Abdel-Halim; Ashraf H Abadi
Journal:  Pharmaceuticals (Basel)       Date:  2022-05-20

2.  Efficient production of α-keto acids by immobilized E. coli-pETduet-1-PmiLAAO in a jacketed packed-bed reactor.

Authors:  Licheng Wu; Xiaolei Guo; Gaobing Wu; Pengfu Liu; Ziduo Liu
Journal:  R Soc Open Sci       Date:  2019-04-24       Impact factor: 2.963

3.  Sulfur(vi) fluoride exchange as a key reaction for synthesizing biaryl sulfate core derivatives as potent hepatitis C virus NS5A inhibitors and their structure-activity relationship studies.

Authors:  Youngsu You; Hee Sun Kim; Jung Woo Park; Gyochang Keum; Sung Key Jang; B Moon Kim
Journal:  RSC Adv       Date:  2018-09-12       Impact factor: 4.036

4.  Liquid crystal nanoparticle formulation as an oral drug delivery system for liver-specific distribution.

Authors:  Dong Ryeol Lee; Ji Su Park; Il Hak Bae; Yan Lee; B Moon Kim
Journal:  Int J Nanomedicine       Date:  2016-03-02

5.  RACK1 mediates rewiring of intracellular networks induced by hepatitis C virus infection.

Authors:  Jae Seung Lee; Keisuke Tabata; Woan-Ing Twu; Md Shafiqur Rahman; Hee Sun Kim; Jin Bae Yu; Min Hyeok Jee; Ralf Bartenschlager; Sung Key Jang
Journal:  PLoS Pathog       Date:  2019-09-16       Impact factor: 6.823
  5 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.