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Effect of lipophilicity modulation on inhibition of human rhinovirus capsid binders |
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| Authors: | Morley Andrew Tomkinson Nicholas Cook Andrew MacDonald Catherine Weaver Richard King Sarah Jenkinson Lesley Unitt John McCrae Christopher Phillips Tim |
| Affiliation: | Department of Chemistry, AstraZeneca R&D Charnwood, Bakewell Road, Loughborough LE11 5RH, UK. andy.morley@astrazeneca.com |
| Abstract: | To try and generate broad spectrum human rhinovirus VP1 inhibitors with more attractive physicochemical, DMPK and safety profiles, we explored the current SAR of known VP1 compounds. This lead to the identification of specific structural regions where reduction in polarity can be achieved, so guiding chemistry to analogues with significantly superior profiles to previously reported inhibitors. |
| Keywords: | VP1 Human rhinovirus Lipophilicity Lipophilic ligand efficiency (LLE) |
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