Low Eddy, Nair Satheesh, Shiau Timothy, Belisle Barbara, Debabov Dmitri, Celeri Chris, Zuck Meghan, Najafi Ron, Georgopapadakou Nafsika, Jain Rakesh
NovaBay Pharmaceuticals Inc, Emeryville, CA 94608, USA.
Bioorg Med Chem Lett. 2009 Jan 1;19(1):196-8. doi: 10.1016/j.bmcl.2008.10.114. Epub 2008 Oct 31.
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.
2-二氯氨基-2-甲基丙烷-1-磺酸钠盐（2a）是内源性N，N-二氯牛磺酸（1）的稳定衍生物，已被鉴定并正在开发为一种局部抗菌剂。研究了类似物的构效关系，以在保持所需稳定性的同时，以最小的哺乳动物毒性实现最佳抗菌活性。所有合成的类似物对金黄色葡萄球菌、大肠杆菌和白色念珠菌的抗菌活性在1-128微克/毫升范围内，对哺乳动物L929细胞的细胞毒性在80-1900微克/毫升范围内。
