N,N-Dichloroaminosulfonic acids as novel topical antimicrobial agents.
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.
Low
Eddy
E
NovaBay Pharmaceuticals Inc, Emeryville, CA 94608, USA.
Nair
Satheesh
S
Shiau
Timothy
T
Belisle
Barbara
B
Debabov
Dmitri
D
Celeri
Chris
C
Zuck
Meghan
M
Najafi
Ron
R
Georgopapadakou
Nafsika
N
Jain
Rakesh
R
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
D000890:Anti-Infective Agents; D000891:Anti-Infective Agents, Local; D013451:Sulfonic Acids; C005741:sulfamic acid