Bioorganic & medicinal chemistry letters · 2013
Sulfonyl-polyol N,N-dichloroamines with rapid, broad-spectrum antimicrobial activity.
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Shiau Timothy P, Low Eddy, Kim Bum, Turtle Eric D, Francavilla Charles, O'Mahony Donogh J R, Friedman Lisa, D'Lima Louisa, Jekle Andreas, Debabov Dmitri, Zuck Meghan, Alvarez Nichole J, Anderson Mark, Najafi Ramin Ron, Jain Rakesh K
Аннотация
The discovery and development of antimicrobial agents that do not give rise to resistance remains an ongoing challenge. Our efforts in this regard continue to reveal new potential therapeutic agents with differing physicochemical properties while retaining the effective N,N-dichloroamine pharmacophore as the key antimicrobial warhead. In this Letter, we disclose agents containing polyol units as a water solubilizing group. These sulfonyl-polyol agents show broad spectrum bactericidal and virucidal activity. These compounds show 1 h MBC's of 16-512 μg/mL against Escherichia coli and 4-256 μg/mL against Staphylococcus aureus at neutral pH, and 1-h IC50's of 4.5-32 μM against Adenovirus 5 and 0.7-3.0 μM against Herpes simplex virus 1. The lead compounds were tested in a tissue culture irritancy assay and showed only minimal irritation at the highest concentrations tested.