| Title | An orally bioavailable oxime ether capsid binder with potent activity against human rhinovirus. | ||
| Author | Watson, Keith G; Brown, Renee N; Cameron, Rachel; Chalmers, David K; Hamilton, Stephanie; Jin, Betty; Krippner, Guy Y; Luttick, Angela; McConnell, Darryl B; Reece, Phillip A; Ryan, Jane; Stanislawski, Pauline C; Tucker, Simon P; Wu, Wen-Yang; Barnard, Dale L; Sidwell, Robert W | ||
| Journal | J Med Chem | Publication Year/Month | 2003-Jul |
| PMID | 12852746 | PMCID | -N/A- |
| Affiliation | 1.Biota Chemistry Laboratory, School of Chemistry, Monash University, PO Box 23 Victoria, Australia 3800. kwatson@wehi.edu.au. | ||
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 IC(50) 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.