title: N,N-Dichloroaminosulfonic acids as novel topical antimicrobial agents.
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 microg/mL and cytotoxicity against mammalian L929 cells in the range 80-1900 microg/mL.
authors.affiliation: NovaBay Pharmaceuticals Inc, Emeryville, CA 94608, USA.
authors.forename: Eddy
authors.initials: E
authors.lastname: Low
authors.forename: Satheesh
authors.initials: S
authors.lastname: Nair
authors.forename: Timothy
authors.initials: T
authors.lastname: Shiau
authors.forename: Barbara
authors.initials: B
authors.lastname: Belisle
authors.forename: Dmitri
authors.initials: D
authors.lastname: Debabov
authors.forename: Chris
authors.initials: C
authors.lastname: Celeri
authors.forename: Meghan
authors.initials: M
authors.lastname: Zuck
authors.forename: Ron
authors.initials: R
authors.lastname: Najafi
authors.forename: Nafsika
authors.initials: N
authors.lastname: Georgopapadakou
authors.forename: Rakesh
authors.initials: R
authors.lastname: Jain
mesh_terms: D000818:Animals; D000890:Anti-Infective Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D000891:Anti-Infective Agents, Local; D002176:Candida albicans / Q000187:drug effects; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D004926:Escherichia coli / Q000187:drug effects; D008826:Microbial Sensitivity Tests; D013211:Staphylococcus aureus / Q000187:drug effects; D013329:Structure-Activity Relationship; D013451:Sulfonic Acids / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D000890:Anti-Infective Agents; D000891:Anti-Infective Agents, Local; D013451:Sulfonic Acids; C005741:sulfamic acid