ACS Medicinal Chemistry Letters

, volume 3 , issue 4 , pages 303-307

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

Susanne C. Feil ¹

Stephanie Hamilton ²

Guy Y. Krippner ²

Bo Lin ²

Angela Luttick ²

Darryl B Mcconnell ²

Roland Nearn ²

Michael Parker ^{1, 3}

Jane Ryan ²

Pauline C. Stanislawski ²

Simon P. Tucker ²

Keith G. Watson ²

CRAIG MORTON ^{1, 2}

Hide authors affiliations Show authors affiliations: 3 affiliations

Biota Structural Biology Laboratory, St. Vincent's Institute, 9 Princes Street, Fitzroy, Victoria 3065, Australia |

Biota Holdings Ltd., 10/585 Blackburn Road, Notting Hill, Victoria 3168, Australia |

Department of Biochemistry and Molecular Biology, Bio21 Molecular Science and Biotechnology Institute, The University of Melbourne, 30 Flemington Road, Parkville, Victoria 3010, Australia |

Publication type: Journal Article

Publication date: 2012-02-16

American Chemical Society (ACS)

ACS Medicinal Chemistry Letters

scimago Q1

wos Q2

SJR: 0.805

CiteScore: 5.8

Impact factor: 4.0

ISSN: 19485875

DOI: 10.1021/ml2002955

Copy DOI

PubMed ID: 24900468

Organic Chemistry

Drug Discovery

Biochemistry

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.

Found

4 citations

Makarov Vadim

🥼 🤝

DSc in Chemistry

177 publications, 4 618 citations, 5 reviews

h-index: 36

Federal Research Centre “Fundamentals of Biotechnology” of the Russian Academy of Sciences

Research interests

Early drug discovery

Medicinal Chemistry

2 citations

Egorova Anna

PhD

22 publications, 270 citations, 23 reviews

h-index: 8

Federal Research Centre “Fundamentals of Biotechnology” of the Russian Academy of Sciences

Research interests

Medicinal Chemistry

1 citation

Galochkina Aнастасия

🤝

PhD in Biological/biomedical sciences

34 publications, 402 citations

h-index: 13

Smorodintsev Research Institute of Influenza

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Cite this

GOST |

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GOST Copy

Feil S. C. et al. An Orally Available 3-Ethoxybenzisoxazole Capsid Binder with Clinical Activity against Human Rhinovirus // ACS Medicinal Chemistry Letters. 2012. Vol. 3. No. 4. pp. 303-307.

GOST all authors (up to 50) Copy

Feil S. C., Hamilton S., Krippner G. Y., Lin B., Luttick A., Mcconnell D. B., Nearn R., Parker M., Ryan J., Stanislawski P. C., Tucker S. P., Watson K. G., MORTON C. An Orally Available 3-Ethoxybenzisoxazole Capsid Binder with Clinical Activity against Human Rhinovirus // ACS Medicinal Chemistry Letters. 2012. Vol. 3. No. 4. pp. 303-307.

RIS |

Cite this

RIS Copy

TY - JOUR

DO - 10.1021/ml2002955

UR - https://doi.org/10.1021/ml2002955

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

T2 - ACS Medicinal Chemistry Letters

AU - Feil, Susanne C.

AU - Hamilton, Stephanie

AU - Krippner, Guy Y.

AU - Lin, Bo

AU - Luttick, Angela

AU - Mcconnell, Darryl B

AU - Nearn, Roland

AU - Parker, Michael

AU - Ryan, Jane

AU - Stanislawski, Pauline C.

AU - Tucker, Simon P.

AU - Watson, Keith G.

AU - MORTON, CRAIG

PY - 2012

DA - 2012/02/16

PB - American Chemical Society (ACS)

SP - 303-307

IS - 4

VL - 3

PMID - 24900468

SN - 1948-5875

ER -

BibTex |

Cite this

BibTex (up to 50 authors) Copy

@article{2012_Feil,

author = {Susanne C. Feil and Stephanie Hamilton and Guy Y. Krippner and Bo Lin and Angela Luttick and Darryl B Mcconnell and Roland Nearn and Michael Parker and Jane Ryan and Pauline C. Stanislawski and Simon P. Tucker and Keith G. Watson and CRAIG MORTON},

title = {An Orally Available 3-Ethoxybenzisoxazole Capsid Binder with Clinical Activity against Human Rhinovirus},

journal = {ACS Medicinal Chemistry Letters},

year = {2012},

volume = {3},

publisher = {American Chemical Society (ACS)},

month = {feb},

url = {https://doi.org/10.1021/ml2002955},

number = {4},

pages = {303--307},

doi = {10.1021/ml2002955}

}

MLA

Cite this

MLA Copy

Feil, Susanne C., et al. “An Orally Available 3-Ethoxybenzisoxazole Capsid Binder with Clinical Activity against Human Rhinovirus.” ACS Medicinal Chemistry Letters, vol. 3, no. 4, Feb. 2012, pp. 303-307. https://doi.org/10.1021/ml2002955.

Publisher

American Chemical Society (ACS)

Journal

ACS Medicinal Chemistry Letters

scimago Q1

wos Q2

SJR

0.805

CiteScore

5.8

Impact factor

4.0

ISSN

19485875 (Print, Electronic)