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N,N-Dichloroaminosulfonic acids as novel topical antimicrobial agents
Authors:Eddy Low  Satheesh Nair  Timothy Shiau  Barbara Belisle  Dmitri Debabov  Chris Celeri  Meghan Zuck  Ron Najafi  Nafsika Georgopapadakou  Rakesh Jain
Institution:NovaBay Pharmaceuticals Inc., 5980 Horton Street, Suite 550, Emeryville, CA 94608, USA
Abstract:2-Dichloroamino-2-methyl-propane-1-sulfonic acid sodium salt (2a), a stable derivative of endogenous N,N-dichlorotaurine (1), has been identified and is under development as a topical antimicrobial agent. Structure–activity relationships of analogs were explored to achieve optimal antimicrobial activity with minimal mammalian toxicity while maintaining the desired stability. All the analogs synthesized showed antimicrobial activity against Staphylococcus aureus, Escherichia coli, and Candida albicans in the range of 1–128 μg/mL and cytotoxicity against mammalian L929 cells in the range 80–1900 μg/mL.
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