Literature DB >> 31303995

Discovery of (aza)indole derivatives as novel respiratory syncytial virus fusion inhibitors.

Xiufang Zheng1, Chungen Liang1, Lisha Wang1, Kun Miao1, Baoxia Wang1, Weixing Zhang1, Dongdong Chen1, Guolong Wu1, Wei Zhu1, Lei Guo1, Song Feng1, Lu Gao1, Hong C Shen1, Hongying Yun1.   

Abstract

A new class of indole derivatives (3) have been identified as potent RSV fusion inhibitors. SAR exploration revealed that 5-Cl and the sulfonyl side chain of the indole scaffold are crucial for anti-RSV activity. Further optimization led to the discovery of a cyclic sulfone (8i) with 2 nM anti-RSV activity and a much improved PK profile compared to the non-cyclic sulfone counterpart.

Entities:  

Year:  2019        PMID： 31303995      PMCID： PMC6596086          DOI： 10.1039/c9md00178f

Source DB:  PubMed          Journal:  Medchemcomm        ISSN： 2040-2503            Impact factor:   3.597


  21 in total

1.  Selection of a respiratory syncytial virus fusion inhibitor clinical candidate. 2. Discovery of a morpholinopropylaminobenzimidazole derivative (TMC353121).

Authors:  Jean-François Bonfanti; Christophe Meyer; Frédéric Doublet; Jérôme Fortin; Philippe Muller; Laurence Queguiner; Tom Gevers; Peggy Janssens; Heidi Szel; Rudy Willebrords; Philip Timmerman; Koen Wuyts; Pieter van Remoortere; Frans Janssens; Piet Wigerinck; Koen Andries
Journal:  J Med Chem       Date:  2008-02-07       Impact factor: 7.446

2.  Fundamental structure-activity relationships associated with a new structural class of respiratory syncytial virus inhibitor.

Authors:  Kuo Long Yu; Yi Zhang; Rita L Civiello; Kathleen F Kadow; Christopher Cianci; Mark Krystal; Nicholas A Meanwell
Journal:  Bioorg Med Chem Lett       Date:  2003-07-07       Impact factor: 2.823

Review 3.  Respiratory syncytial virus infection: clinical features, management, and prophylaxis.

Authors:  Anne Greenough
Journal:  Curr Opin Pulm Med       Date:  2002-05       Impact factor: 3.155

Review 4.  WITHDRAWN: Ribavirin for respiratory syncytial virus infection of the lower respiratory tract in infants and young children.

Authors:  Kathleen Ventre; Adrienne Randolph
Journal:  Cochrane Database Syst Rev       Date:  2010-05-12

5.  Respiratory syncytial virus fusion inhibitors. Part 4: optimization for oral bioavailability.

Authors:  Kuo-Long Yu; Ny Sin; Rita L Civiello; X Alan Wang; Keith D Combrink; H Belgin Gulgeze; Brian L Venables; J J Kim Wright; Richard A Dalterio; Lisa Zadjura; Anthony Marino; Sandra Dando; Celia D'Arienzo; Kathleen F Kadow; Christopher W Cianci; Zhufang Li; Junius Clarke; Eugene V Genovesi; Ivette Medina; Lucinda Lamb; Richard J Colonno; Zheng Yang; Mark Krystal; Nicholas A Meanwell
Journal:  Bioorg Med Chem Lett       Date:  2006-12-01       Impact factor: 2.823

6.  Substituted benzimidazoles with nanomolar activity against respiratory syncytial virus.

Authors:  Koen Andries; Marc Moeremans; Tom Gevers; Rudy Willebrords; Cois Sommen; Jean Lacrampe; Frans Janssens; Philip R Wyde
Journal:  Antiviral Res       Date:  2003-11       Impact factor: 5.970

7.  Inhibition of respiratory syncytial virus fusion by the small molecule VP-14637 via specific interactions with F protein.

Authors:  Janet L Douglas; Marites L Panis; Edmund Ho; Kuei-Ying Lin; Steve H Krawczyk; Deborah M Grant; Ruby Cai; Swami Swaminathan; Tomas Cihlar
Journal:  J Virol       Date:  2003-05       Impact factor: 5.103

8.  Orally active fusion inhibitor of respiratory syncytial virus.

Authors:  Christopher Cianci; Kuo-Long Yu; Keith Combrink; Ny Sin; Bradley Pearce; Alan Wang; Rita Civiello; Stacey Voss; Guangxiang Luo; Kathy Kadow; Eugene V Genovesi; Brian Venables; Hatice Gulgeze; Ashok Trehan; Jennifer James; Lucinda Lamb; Ivette Medina; Julia Roach; Zheng Yang; Lisa Zadjura; Richard Colonno; Junius Clark; Nicholas Meanwell; Mark Krystal
Journal:  Antimicrob Agents Chemother       Date:  2004-02       Impact factor: 5.191

Review 9.  Respiratory syncytial virus--a comprehensive review.

Authors:  Andrea T Borchers; Christopher Chang; M Eric Gershwin; Laurel J Gershwin
Journal:  Clin Rev Allergy Immunol       Date:  2013-12       Impact factor: 8.667

Review 10.  Respiratory syncytial virus entry inhibitors targeting the F protein.

Authors:  Zhiwu Sun; Yanbin Pan; Shibo Jiang; Lu Lu
Journal:  Viruses       Date:  2013-01-16       Impact factor: 5.048
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