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

作者：Feil Susanne C; Hamilton Stephanie; Krippner Guy Y; Lin Bo; Luttick Angela; McConnell Darryl B; Nearn Roland; Parker Michael W; Ryan Jane; Stanislawski Pauline C; Tucker Simon P; Watson Keith G; Morton Craig J

来源：ACS Medicinal Chemistry Letters, 2012, 3(4): 303-307.

DOI：10.1021/ml2002955

• antiviral
• rhinovirus
• capsid
• inhibitor

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.

• 出版日期2012-4