Literature DB >> 24900468

An Orally Available 3-Ethoxybenzisoxazole Capsid Binder with Clinical Activity against Human Rhinovirus.

Susanne C Feil1, Stephanie Hamilton2, Guy Y Krippner2, Bo Lin2, Angela Luttick2, Darryl B McConnell2, Roland Nearn2, Michael W Parker3, Jane Ryan2, Pauline C Stanislawski2, Simon P Tucker2, Keith G Watson2, Craig J Morton4.   

Abstract

Respiratory infections caused by human rhinovirus are responsible for severe exacerbations of underlying clinical conditions such as asthma in addition to their economic cost in terms of lost working days due to illness. While several antiviral compounds for treating rhinoviral infections have been discovered, none have succeeded, to date, in reaching approval for clinical use. We have developed a potent, orally available rhinovirus inhibitor 6 that has progressed through early clinical trials. The compound shows favorable pharmacokinetic and activity profiles and has a confirmed mechanism of action through crystallographic studies of a rhinovirus-compound complex. The compound has now progressed to phase IIb clinical studies of its effect on natural rhinovirus infection in humans.

Entities:  

Keywords:  antiviral; capsid; inhibitor; rhinovirus

Year:  2012        PMID： 24900468      PMCID： PMC4025830          DOI： 10.1021/ml2002955

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


  23 in total

1.  Pharmacokinetics and safety of an antirhinoviral agent, ruprintrivir, in healthy volunteers.

Authors:  Poe-Hirr Hsyu; Yazdi K Pithavala; Merril Gersten; Carol A Penning; Bradley M Kerr
Journal:  Antimicrob Agents Chemother       Date:  2002-02       Impact factor: 5.191

2.  Relationship of pleconaril susceptibility and clinical outcomes in treatment of common colds caused by rhinoviruses.

Authors:  Daniel C Pevear; Frederick G Hayden; Tina M Demenczuk; Linda R Barone; Mark A McKinlay; Marc S Collett
Journal:  Antimicrob Agents Chemother       Date:  2005-11       Impact factor: 5.191

3.  Intranasal pirodavir (R77,975) treatment of rhinovirus colds.

Authors:  F G Hayden; G J Hipskind; D H Woerner; G F Eisen; M Janssens; P A Janssen; K Andries
Journal:  Antimicrob Agents Chemother       Date:  1995-02       Impact factor: 5.191

4.  Activity of pleconaril against enteroviruses.

Authors:  D C Pevear; T M Tull; M E Seipel; J M Groarke
Journal:  Antimicrob Agents Chemother       Date:  1999-09       Impact factor: 5.191

Review 5.  Selective inhibitors of picornavirus replication.

Authors:  Armando M De Palma; Inge Vliegen; Erik De Clercq; Johan Neyts
Journal:  Med Res Rev       Date:  2008-11       Impact factor: 12.944

6.  An orally bioavailable oxime ether capsid binder with potent activity against human rhinovirus.

Authors:  Keith G Watson; Renee N Brown; Rachel Cameron; David K Chalmers; Stephanie Hamilton; Betty Jin; Guy Y Krippner; Angela Luttick; Darryl B McConnell; Phillip A Reece; Jane Ryan; Pauline C Stanislawski; Simon P Tucker; Wen-Yang Wu; Dale L Barnard; Robert W Sidwell
Journal:  J Med Chem       Date:  2003-07-17       Impact factor: 7.446

7.  Phase II, randomized, double-blind, placebo-controlled studies of ruprintrivir nasal spray 2-percent suspension for prevention and treatment of experimentally induced rhinovirus colds in healthy volunteers.

Authors:  Frederick G Hayden; Ronald B Turner; Jack M Gwaltney; Kathy Chi-Burris; Merril Gersten; Poe Hsyu; Amy K Patick; George J Smith; Leora S Zalman
Journal:  Antimicrob Agents Chemother       Date:  2003-12       Impact factor: 5.191

8.  Safety and efficacy of intranasal pirodavir (R77975) in experimental rhinovirus infection.

Authors:  F G Hayden; K Andries; P A Janssen
Journal:  Antimicrob Agents Chemother       Date:  1992-04       Impact factor: 5.191

Review 9.  Rhinovirus chemotherapy.

Authors:  Amy K Patick
Journal:  Antiviral Res       Date:  2006-04-18       Impact factor: 5.970

10.  Efficacy and safety of oral pleconaril for treatment of colds due to picornaviruses in adults: results of 2 double-blind, randomized, placebo-controlled trials.

Authors:  Frederick G Hayden; Darrell T Herrington; Teresa L Coats; Kenneth Kim; Ellen C Cooper; Stephen A Villano; Siyu Liu; Spencer Hudson; Daniel C Pevear; Marc Collett; Mark McKinlay
Journal:  Clin Infect Dis       Date:  2003-06-06       Impact factor: 9.079
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  14 in total

1.  Phosphatidylinositol 4-kinase III beta is essential for replication of human rhinovirus and its inhibition causes a lethal phenotype in vivo.

Authors:  Catherine Spickler; Julie Lippens; Marie-Kristine Laberge; Sophie Desmeules; Édith Bellavance; Michel Garneau; Tim Guo; Oliver Hucke; Pieter Leyssen; Johan Neyts; Fréderic H Vaillancourt; Anne Décor; Jeff O'Meara; Michael Franti; Annick Gauthier
Journal:  Antimicrob Agents Chemother       Date:  2013-05-06       Impact factor: 5.191

2.  Identification of a series of compounds with potent antiviral activity for the treatment of enterovirus infections.

Authors:  Angus M MacLeod; Dale R Mitchell; Nicholas J Palmer; Hervé Van de Poël; Katja Conrath; Martin Andrews; Pieter Leyssen; Johan Neyts
Journal:  ACS Med Chem Lett       Date:  2013-05-08       Impact factor: 4.345

3.  3-Aryl-1,2,4-oxadiazole Derivatives Active Against Human Rhinovirus.

Authors:  Jinwoo Kim; Jin Soo Shin; Sunjoo Ahn; Soo Bong Han; Young-Sik Jung
Journal:  ACS Med Chem Lett       Date:  2018-04-13       Impact factor: 4.345

4.  Novel capsid binder and PI4KIIIbeta inhibitors for EV-A71 replication inhibition.

Authors:  Yong Wah Tan; Wan Keat Yam; Rachel Jia Wen Kooi; Jacob Westman; Gustav Arbrandt; Justin Jang Hann Chu
Journal:  Sci Rep       Date:  2021-05-06       Impact factor: 4.379

5.  In vitro characterisation of a pleconaril/pirodavir-like compound with potent activity against rhinoviruses.

Authors:  Céline Lacroix; Samuela Laconi; Fabrizio Angius; Antonio Coluccia; Romano Silvestri; Raffaello Pompei; Johan Neyts; Pieter Leyssen
Journal:  Virol J       Date:  2015-07-14       Impact factor: 4.099

6.  More-powerful virus inhibitors from structure-based analysis of HEV71 capsid-binding molecules.

Authors:  Luigi De Colibus; Xiangxi Wang; John A B Spyrou; James Kelly; Jingshan Ren; Jonathan Grimes; Gerhard Puerstinger; Nicola Stonehouse; Thomas S Walter; Zhongyu Hu; Junzhi Wang; Xuemei Li; Wei Peng; David Rowlands; Elizabeth E Fry; Zihe Rao; David I Stuart
Journal:  Nat Struct Mol Biol       Date:  2014-02-09       Impact factor: 15.369

7.  Potent antiviral agents fail to elicit genetically-stable resistance mutations in either enterovirus 71 or Coxsackievirus A16.

Authors:  James T Kelly; Luigi De Colibus; Lauren Elliott; Elizabeth E Fry; David I Stuart; David J Rowlands; Nicola J Stonehouse
Journal:  Antiviral Res       Date:  2015-10-30       Impact factor: 5.970

8.  Pyrazolopyrimidines: Potent Inhibitors Targeting the Capsid of Rhino- and Enteroviruses.

Authors:  Vadim A Makarov; Heike Braun; Martina Richter; Olga B Riabova; Johannes Kirchmair; Elena S Kazakova; Nora Seidel; Peter Wutzler; Michaela Schmidtke
Journal:  ChemMedChem       Date:  2015-08-10       Impact factor: 3.466

Review 9.  Antiviral therapeutic approaches for human rhinovirus infections.

Authors:  Victor Casanova; Filipa H Sousa; Craig Stevens; Peter G Barlow
Journal:  Future Virol       Date:  2018-06-12       Impact factor: 1.831

Review 10.  Toward antiviral therapy/prophylaxis for rhinovirus-induced exacerbations of chronic obstructive pulmonary disease: challenges, opportunities, and strategies.

Authors:  Hendrik Jan Thibaut; Céline Lacroix; Armando M De Palma; David Franco; Mark Decramer; Johan Neyts
Journal:  Rev Med Virol       Date:  2015-09-21       Impact factor: 6.989
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