N,N-Dichloroaminosulfonic acids as novel topical antimicrobial agents |
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Authors: | Eddy Low Satheesh Nair Timothy Shiau Barbara Belisle Dmitri Debabov Chris Celeri Meghan Zuck Ron Najafi Nafsika Georgopapadakou Rakesh Jain |
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Affiliation: | NovaBay Pharmaceuticals Inc., 5980 Horton Street, Suite 550, Emeryville, CA 94608, USA |
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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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