Twenty-one mono- and biscationic quaternary ammonium amphiphiles (monoQACs and bisQACs) were rapidly prepared in order to investigate the effects of rigidity of a diamine core structure on antiseptic activity. As anticipated, the bioactivity against a panel of six bacteria including methicillin-resistant Staphylococcus aureus (MRSA) strains was strong for bisQAC structures, and is clearly correlated with the length of non-polar side chains. Modest advantages were noted for amide-containing side chains, as compared with straight-chained alkyl substituents. Surprisingly, antiseptics with more rigidly disposed side chains, such as those in DABCO-12,12, showed the highest level of antimicrobial activity, with single-digit MIC values or better against the entire bacterial panel, including sub-micromolar activity against an MRSA strain.

中文翻译：

---

BisQAC两亲型防腐剂刚性-活性关系的调查。

为了研究二胺核心结构的刚度对杀菌活性的影响，迅速制备了21个单阳离子和双阳离子季铵两亲物（monoQAC和bisQAC）。如预期的那样，对包括耐甲氧西林的金黄色葡萄球菌（MRSA）菌株在内的六种细菌的生物活性对于bisQAC结构很强，并且显然与非极性侧链的长度相关。与直链烷基取代基相比，含酰胺侧链的优势不大。出乎意料的是，侧链配置更严格的防腐剂（例如DABCO-12,12中的那些）显示出最高水平的抗菌活性，对整个细菌群体的MIC值为一位数或更高，包括对MRSA的亚微摩尔活性。拉紧。