An orally bioavailable oxime ether capsid binder with potent activity against human rhinovirus
- Author(s)
- Watson, KG; Brown, RN; Cameron, R; Chalmers, DK; Hamilton, S; Jin, B; Krippner, GY; Luttick, A; McConnell, DB; Reece, PA; Ryan, J; Stanislawski, PC; Tucker, SP; Wu, WY; Barnard, DL; Sidwell, RW;
- Details
- Publication Year 2003-07-17,Volume 46,Issue #15,Page 3181-3184
- Journal Title
- JOURNAL OF MEDICINAL CHEMISTRY
- Publication Type
- Journal Article
- 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.
- Publisher
- AMER CHEMICAL SOC
- Keywords
- COMMON COLD; ANTIVIRAL COMPOUNDS; DESIGN; INHIBITORS; AGENTS
- Publisher's Version
- https://doi.org/10.1021/jm0202876
- Terms of Use/Rights Notice
- Refer to copyright notice on published article.
Creation Date: 2003-07-17 12:00:00