An optimization campaign focused on improving pharmacological activity and physicochemical properties of a recently-identified class of cyclosulfamide-based norovirus inhibitors has been carried out. Dimeric compound 4 was found to be a ∼10-fold more potent norovirus inhibitor (ED(50) 0.4 μM) compared to the original hit, however, isonipecotic acid ester derivatives 7e and 10a were shown to have superior therapeutic indices.
Download full-text PDF |
Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3259182 | PMC |
| http://dx.doi.org/10.1016/j.ejmech.2011.10.019 | DOI Listing |
Publication Analysis
Top Keywords
cyclosulfamide-based derivatives
4
derivatives inhibitors
4
inhibitors noroviruses
4
noroviruses optimization
4
optimization campaign
4
campaign focused
4
focused improving
4
improving pharmacological
4
pharmacological activity
4
activity physicochemical
4
Similar Publications
Want AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!