Article
An Orally Bioavailable Oxime Ether Capsid Binder with Potent Activity against Human Rhinovirus
Journal of Medicinal Chemistry
Document Type
Article
Publisher
American Chemical Society
Publication Date
1-1-2003
Disciplines
Abstract
A series of capsid-binding compounds was screened against human rhinovirus (HRV) using a CPE based assay. The ethyl oxime ether 14 was found to have outstanding anti-HRV activity (median IC50 4.75 ng/mL), and unlike the equivalent ethyl ester compound 3 (Pirodavir), it has good oral bioavailability, making it a promising development candidate. Compound 14 illustrates that an oxime ether group can act as a metabolically stable bioisostere for an ester functionality.
Citation Information
Watson, K.G., Brown, R.N., Cameron, R., Chalmers, D.K., Hamilton, S., Jin, B., Krippner, G.Y., Luttick,....Barnard, D.L., Sidwell, R.W 2003. An orally bioavailable oxime ether capsid binder with potent activity against human rhinovirus. Journal of Medicinal Chemistry, 46(15): 3181-3184.
Originally published by the American Chemical Society. Publisher's PDF and HTML fulltext available through remote link.