Literature DB >> 18947995

Non-nucleoside inhibitors of the hepatitis C virus NS5B RNA-dependant RNA polymerase: 2-aryl-3-heteroaryl-1,3-thiazolidin-4-one derivatives.

Ravindra K Rawal1, S B Katti, Neerja Kaushik-Basu, Payal Arora, Zhenhua Pan.   

Abstract

Hepatitis C virus (HCV) NS5B RNA polymerase is crucial for replicating the HCV RNA genome and is an attractive target for developing anti-HCV drugs. A novel series of 2,3-diaryl-1,3-thiazolidin-4-one derivatives were evaluated for their ability to inhibit HCV NS5B. Of this series, compounds 4c, 5b, 5c and 6 emerged as more potent, displaying over 95% inhibition of NS5B RNA polymerase activity in vitro. The two most active compounds 4c and 5c exhibited an IC(50) of 31.9 microM and 32.2 microM, respectively, against HCV NS5B.

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Year:  2008        PMID: 18947995      PMCID: PMC2604905          DOI: 10.1016/j.bmcl.2008.10.023

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


  32 in total

Review 1.  Overview of hepatitis C virus genome structure, polyprotein processing, and protein properties.

Authors:  K E Reed; C M Rice
Journal:  Curr Top Microbiol Immunol       Date:  2000       Impact factor: 4.291

2.  Synthesis, characterisation and biological activity of novel 4-thiazolidinones, 1,3,4-oxadiazoles and some related compounds.

Authors:  S Güniz Küçükgüzel; E Elçin Oruç; Sevim Rollas; Fikrettin Sahin; Ahmet Ozbek
Journal:  Eur J Med Chem       Date:  2002-03       Impact factor: 6.514

3.  Synthesis of some new triazoles as potential antifungal agents.

Authors:  H T Fahmy
Journal:  Boll Chim Farm       Date:  2001 Nov-Dec

4.  Design, synthesis, structure-activity relationships, and molecular modeling studies of 2,3-diaryl-1,3-thiazolidin-4-ones as potent anti-HIV agents.

Authors:  Maria L Barreca; Jan Balzarini; Alba Chimirri; Erik De Clercq; Laura De Luca; Hans Dieter Höltje; Monika Höltje; Anna Maria Monforte; Pietro Monforte; Christophe Pannecouque; Angela Rao; Maria Zappalà
Journal:  J Med Chem       Date:  2002-11-21       Impact factor: 7.446

5.  Discovery of 2,3-diaryl-1,3-thiazolidin-4-ones as potent anti-HIV-1 agents.

Authors:  M L Barreca; A Chimirri; L De Luca; A M Monforte; P Monforte; A Rao; M Zappalà; J Balzarini; E De Clercq; C Pannecouque; M Witvrouw
Journal:  Bioorg Med Chem Lett       Date:  2001-07-09       Impact factor: 2.823

Review 6.  Understanding hepatitis C.

Authors:  John G McHutchison
Journal:  Am J Manag Care       Date:  2004-03       Impact factor: 2.229

7.  Synthesis and antituberculosis activity of cycloalkylidenehydrazide and 4-aza-1-thiaspiro[4.5]decan-3-one derivatives of imidazo[2,1-b]thiazole.

Authors:  Nuray Ulusoy
Journal:  Arzneimittelforschung       Date:  2002

8.  Novel inhibitors of an emerging target in Mycobacterium tuberculosis; substituted thiazolidinones as inhibitors of dTDP-rhamnose synthesis.

Authors:  Kerim Babaoglu; Mark A Page; Victoria C Jones; Michael R McNeil; Changjiang Dong; James H Naismith; Richard E Lee
Journal:  Bioorg Med Chem Lett       Date:  2003-10-06       Impact factor: 2.823

Review 9.  Targeting NS5B RNA-dependent RNA polymerase for anti-HCV chemotherapy.

Authors:  Jim Zhen Wu; Zhi Hong
Journal:  Curr Drug Targets Infect Disord       Date:  2003-09

10.  4-Thiazolidinones: a novel class of hepatitis C virus NS5B polymerase inhibitors.

Authors:  Neerja Kaushik-Basu; Alain Bopda-Waffo; Tanaji T Talele; Amartya Basu; Ye Chen; S Guniz Kucukguzel
Journal:  Front Biosci       Date:  2008-05-01
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  6 in total

1.  Design, synthesis and in silico screening of benzoxazole-thiazolidinone hybrids as potential inhibitors of SARS-CoV-2 proteases.

Authors:  Vijay Sai Krishna Cheerala; Prasanth Ghanta; Sundaresan Chittor Neelakantan
Journal:  RSC Adv       Date:  2021-12-10       Impact factor: 4.036

2.  Crystal structure of (±)-3-[(benzo[d][1,3]dioxol-5-yl)meth-yl]-2-(3,4,5-tri-meth-oxy-phen-yl)-1,3-thia-zolidin-4-one.

Authors:  Rodolfo Moreno-Fuquen; Juan C Castillo; Rodrigo Abonia; Javier Ellena; Carlos A De Simone
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2014-11-05

3.  Dual inhibitors of hepatitis C virus and hepatocellular carcinoma: design, synthesis and docking studies.

Authors:  Mostafa Mm El-Miligy; Samia M Rida; Fawzia A Ashour; Mona H Badr; Ehab M El-Bassiony; Maha A El-Demellawy; Ashraf M Omar
Journal:  Future Sci OA       Date:  2017-10-25

Review 4.  5-Ene-4-thiazolidinones - An efficient tool in medicinal chemistry.

Authors:  Danylo Kaminskyy; Anna Kryshchyshyn; Roman Lesyk
Journal:  Eur J Med Chem       Date:  2017-09-20       Impact factor: 6.514

5.  2-Heteroarylimino-5-arylidene-4-thiazolidinones as a new class of non-nucleoside inhibitors of HCV NS5B polymerase.

Authors:  Ilkay Küçükgüzel; Gökhan Satılmış; K R Gurukumar; Amartya Basu; Esra Tatar; Daniel B Nichols; Tanaji T Talele; Neerja Kaushik-Basu
Journal:  Eur J Med Chem       Date:  2013-09-12       Impact factor: 6.514

6.  Synthesis and biological activity evaluation of 5-pyrazoline substituted 4-thiazolidinones.

Authors:  Dmytro Havrylyuk; Borys Zimenkovsky; Olexandr Vasylenko; Craig W Day; Donald F Smee; Philippe Grellier; Roman Lesyk
Journal:  Eur J Med Chem       Date:  2013-06-06       Impact factor: 6.514

  6 in total

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