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An orally bioavailable oxime ether capsid binder with potent activity against human rhinovirus |
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| Authors: | 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 |
| Institution: | Biota Chemistry Laboratory, School of Chemistry, Monash University, PO Box 23 Victoria, Australia 3800. kwatson@wehi.edu.au |
| 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 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. |
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