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

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• 作者：Susanne C. Feil ; Stephanie Hamilton ; Guy Y. Krippner ; Bo Lin ; Angela Luttick ; Darryl B. McConnell ; Roland Nearn ; Michael W. Parker ; Jane Ryan ; Pauline C. Stanislawski ; Simon P. Tucker ; Keith G. Watson ; Craig J. Morton
• 刊名：ACS Medicinal Chemistry Letters
• 出版年：2012
• 出版时间：April 12, 2012
• 年：2012
• 卷：3
• 期：4
• 页码：303-307
• 全文大小：304K
• 年卷期：v.3,no.4(April 12, 2012)
• ISSN：1948-5875

文摘

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鈭抍ompound complex. The compound has now progressed to phase IIb clinical studies of its effect on natural rhinovirus infection in humans.

Keywords:

antiviral; rhinovirus; capsid; inhibitor