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Further Investigations into Rigidity-Activity Relationships in BisQAC Amphiphilic Antiseptics.
ChemMedChem ( IF 3.4 ) Pub Date : 2020-02-11 , DOI: 10.1002/cmdc.201900662
Austin J Leitgeb 1 , Javier A Feliciano 1 , Hugo A Sanchez 1 , Ryan A Allen 2 , Kelly R Morrison 2 , Kyle J Sommers 1 , Robert G Carden 1 , William M Wuest 2 , Kevin P C Minbiole 1
Affiliation  

Thirty-six biscationic quaternary ammonium compounds were efficiently synthesized in one step to examine the effect of molecular geometry of two-carbon linkers on antimicrobial activity. The synthesized compounds showed strong antimicrobial activity against a panel of both Gram-positive and Gram-negative bacteria, including methicillin-resistant Staphylococcus aureus (MRSA). While the linker geometry showed only a modest correlation with antimicrobial activity, several of the synthesized bisQACs are promising potential antiseptics due to good antimicrobial activity (MIC≤2 μM) and their higher therapeutic indices compared to previously reported QACs.

中文翻译:

BisQAC 两亲性防腐剂刚性-活性关系的进一步研究。

一步有效合成了 36 种双阳离子季铵化合物,以研究双碳连接体的分子几何形状对抗菌活性的影响。合成的化合物对一系列革兰氏阳性和革兰氏阴性细菌(包括耐甲氧西林金黄色葡萄球菌(MRSA))表现出强大的抗菌活性。虽然连接体几何形状与抗菌活性仅表现出适度的相关性,但由于良好的抗菌活性(MIC≤2μM)以及与之前报道的 QAC 相比更高的治疗指数,几种合成的 bisQAC 是有前途的潜在防腐剂。
更新日期:2020-02-11
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