Literature DB >> 31493987

Novel influenza polymerase PB2 inhibitors for the treatment of influenza A infection.

Hongwang Zhang1, Longhu Zhou1, Sarah Amichai1, Keivan Zandi1, Bryan Cox1, Raymond Schinazi1, Franck Amblard2.   

Abstract

Exploration of the chemical space of known influenza polymerase PB2 inhibitor Pimodivir, was performed by our group. We synthesized and identified compounds 16a and 16b, two novel thienopyrimidine derivatives displaying anti-influenza A activity in the single digit nanomolar range in cell culture. Binding of these unique compounds in the influenza polymerase PB2 pocket was also determined using molecular modeling.
Copyright © 2019 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Antiviral; Flu; Influenza A; Virus

Mesh：

Substances：

Year:  2019        PMID： 31493987      PMCID： PMC7732027          DOI： 10.1016/j.bmcl.2019.126639

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  13 in total

1.  Novel procedure for modeling ligand/receptor induced fit effects.

Authors:  Woody Sherman; Tyler Day; Matthew P Jacobson; Richard A Friesner; Ramy Farid
Journal:  J Med Chem       Date:  2006-01-26       Impact factor: 7.446

2.  Use of an induced fit receptor structure in virtual screening.

Authors:  Woody Sherman; Hege S Beard; Ramy Farid
Journal:  Chem Biol Drug Des       Date:  2006-01       Impact factor: 2.817

3.  The Next Wave of Influenza Drugs.

Authors:  Megan L Shaw
Journal:  ACS Infect Dis       Date:  2017-09-11       Impact factor: 5.084

4.  Phase 2b Study of Pimodivir (JNJ-63623872) as Monotherapy or in Combination With Oseltamivir for Treatment of Acute Uncomplicated Seasonal Influenza A: TOPAZ Trial.

Authors:  Robert W Finberg; Riin Lanno; David Anderson; Roman Fleischhackl; Wilbert van Duijnhoven; Robert S Kauffman; Teddy Kosoglou; Johan Vingerhoets; Lorant Leopold
Journal:  J Infect Dis       Date:  2019-03-15       Impact factor: 5.226

5.  Incidence of adamantane resistance among influenza A (H3N2) viruses isolated worldwide from 1994 to 2005: a cause for concern.

Authors:  Rick A Bright; Marie-jo Medina; Xiyan Xu; Gilda Perez-Oronoz; Teresa R Wallis; Xiaohong M Davis; Laura Povinelli; Nancy J Cox; Alexander I Klimov
Journal:  Lancet       Date:  2005-09-22       Impact factor: 79.321

Review 6.  Inhibitors of Influenza A Virus Polymerase.

Authors:  Shuofeng Yuan; Lei Wen; Jie Zhou
Journal:  ACS Infect Dis       Date:  2018-01-22       Impact factor: 5.084

7.  Discovery of a novel, first-in-class, orally bioavailable azaindole inhibitor (VX-787) of influenza PB2.

Authors:  Michael P Clark; Mark W Ledeboer; Ioana Davies; Randal A Byrn; Steven M Jones; Emanuele Perola; Alice Tsai; Marc Jacobs; Kwame Nti-Addae; Upul K Bandarage; Michael J Boyd; Randy S Bethiel; John J Court; Hongbo Deng; John P Duffy; Warren A Dorsch; Luc J Farmer; Huai Gao; Wenxin Gu; Katrina Jackson; Dylan H Jacobs; Joseph M Kennedy; Brian Ledford; Jianglin Liang; François Maltais; Mark Murcko; Tiansheng Wang; M Woods Wannamaker; Hamilton B Bennett; Joshua R Leeman; Colleen McNeil; William P Taylor; Christine Memmott; Min Jiang; Rene Rijnbrand; Christopher Bral; Ursula Germann; Azin Nezami; Yuegang Zhang; Francesco G Salituro; Youssef L Bennani; Paul S Charifson
Journal:  J Med Chem       Date:  2014-07-24       Impact factor: 7.446

8.  Emergence and spread of oseltamivir-resistant A(H1N1) influenza viruses in Oceania, South East Asia and South Africa.

Authors:  Aeron C Hurt; Joanne Ernest; Yi-Mo Deng; Pina Iannello; Terry G Besselaar; Chris Birch; Philippe Buchy; Malinee Chittaganpitch; Shu-Chun Chiu; Dominic Dwyer; Aurélie Guigon; Bruce Harrower; Ip Peng Kei; Tuckweng Kok; Cui Lin; Ken McPhie; Apandi Mohd; Remigio Olveda; Tony Panayotou; William Rawlinson; Lesley Scott; David Smith; Holly D'Souza; Naomi Komadina; Robert Shaw; Anne Kelso; Ian G Barr
Journal:  Antiviral Res       Date:  2009-03-24       Impact factor: 5.970

9.  Pimodivir treatment in adult volunteers experimentally inoculated with live influenza virus: a Phase IIa, randomized, double-blind, placebo-controlled study.

Authors:  Jose M Trevejo; Mohammed Asmal; Johan Vingerhoets; Ramon Polo; Sarah Robertson; Ying Jiang; Tara L Kieffer; Lorant Leopold
Journal:  Antivir Ther       Date:  2018

10.  Characterization of influenza virus variants induced by treatment with the endonuclease inhibitor baloxavir marboxil.

Authors:  Shinya Omoto; Valentina Speranzini; Takashi Hashimoto; Takeshi Noshi; Hiroto Yamaguchi; Makoto Kawai; Keiko Kawaguchi; Takeki Uehara; Takao Shishido; Akira Naito; Stephen Cusack
Journal:  Sci Rep       Date:  2018-06-25       Impact factor: 4.379
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  2 in total

Review 1.  Contemporary medicinal chemistry strategies for the discovery and optimization of influenza inhibitors targeting vRNP constituent proteins.

Authors:  Lingxin Hou; Ying Zhang; Han Ju; Srinivasulu Cherukupalli; Ruifang Jia; Jian Zhang; Bing Huang; Arianna Loregian; Xinyong Liu; Peng Zhan
Journal:  Acta Pharm Sin B       Date:  2021-11-19       Impact factor: 14.903

Review 2.  Thienopyrimidine: A Promising Scaffold to Access Anti-Infective Agents.

Authors:  Prisca Lagardère; Cyril Fersing; Nicolas Masurier; Vincent Lisowski
Journal:  Pharmaceuticals (Basel)       Date:  2021-12-27
  2 in total

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