Literature DB >> 22578461

Synthesis and characterization of 2'-C-Me branched C-nucleosides as HCV polymerase inhibitors.

Aesop Cho1, Lijun Zhang, Jie Xu, Darius Babusis, Thomas Butler, Rick Lee, Oliver L Saunders, Ting Wang, Jay Parrish, Jason Perry, Joy Y Feng, Adrian S Ray, Choung U Kim.   

Abstract

A series of 2'-C-methyl branched purine and pyrimidine C-nucleosides were prepared. Their anti-HCV activity and pharmacological properties were profiled, and compared with known 2'-C-Me N-nucleoside counterparts. In particular, 2'-C-Me 4-aza-7,9-dideazaadenosine C-nucleoside (2) was found to have potent and selective anti-HCV activity in vitro as well as a favorable pharmacokinetic profile and in vivo potential for enhanced potency over the corresponding N-nucleoside.
Copyright © 2012 Elsevier Ltd. All rights reserved.

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Year:  2012        PMID: 22578461     DOI: 10.1016/j.bmcl.2012.04.065

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


  5 in total

1.  Discovery and Synthesis of C-Nucleosides as Potential New Anti-HCV Agents.

Authors:  Alistair G Draffan; Barbara Frey; Brett Pool; Carlie Gannon; Edward M Tyndall; Michael Lilly; Paula Francom; Richard Hufton; Rosliana Halim; Saba Jahangiri; Silas Bond; Van T T Nguyen; Tyrone P Jeynes; Veronika Wirth; Angela Luttick; Danielle Tilmanis; Jesse D Thomas; Melinda Pryor; Kate Porter; Craig J Morton; Bo Lin; Jianmin Duan; George Kukolj; Bruno Simoneau; Ginette McKercher; Lisette Lagacé; Ma'an Amad; Richard C Bethell; Simon P Tucker
Journal:  ACS Med Chem Lett       Date:  2014-04-10       Impact factor: 4.345

2.  Remdesivir (GS-5734) Impedes Enterovirus Replication Through Viral RNA Synthesis Inhibition.

Authors:  Wei Ye; Min Yao; Yangchao Dong; Chuantao Ye; Dan Wang; He Liu; Hongwei Ma; Hui Zhang; Libin Qi; Yuewu Yang; Yuan Wang; Liang Zhang; Linfeng Cheng; Xin Lv; Zhikai Xu; Yingfeng Lei; Fanglin Zhang
Journal:  Front Microbiol       Date:  2020-06-12       Impact factor: 5.640

3.  Synthesis, Kinetic and Conformational Studies of 2-Substituted-5-(β-d-glucopyranosyl)-pyrimidin-4-ones as Potential Inhibitors of Glycogen Phosphorylase.

Authors:  Konstantinos F Mavreas; Dionysios D Neofytos; Evangelia D Chrysina; Alessandro Venturini; Thanasis Gimisis
Journal:  Molecules       Date:  2020-11-22       Impact factor: 4.411

Review 4.  Reviews on Biological Activity, Clinical Trial and Synthesis Progress of Small Molecules for the Treatment of COVID-19.

Authors:  Dingzhong Li; Jianbing Hu; Dian Li; Weijun Yang; Shuang-Feng Yin; Renhua Qiu
Journal:  Top Curr Chem (Cham)       Date:  2021-01-11

Review 5.  Recent advances in synthetic approaches for medicinal chemistry of C-nucleosides.

Authors:  Kartik Temburnikar; Katherine L Seley-Radtke
Journal:  Beilstein J Org Chem       Date:  2018-04-05       Impact factor: 2.883

  5 in total

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