脱氢乙酸烯胺衍生物的合成及其抗菌活性
Synthesis and antibacterial activities of enamine derivatives of dehydroacetic acid.
作者信息
Baldwin Alex G, Bevan Jonathan, Brough David, Ledder Ruth, Freeman Sally
机构信息
1Division of Pharmacy and Optometry, School of Health Sciences, Faculty of Biology, Medicine and Health, Manchester Academic Health Science Centre, The University of Manchester, Stopford Building, Oxford Road, Manchester, M13 9PT UK.
2Division of Neuroscience and Experimental Psychology, School of Biological Sciences, Faculty of Biology, Medicine and Health, Manchester Academic Health Science Centre, The University of Manchester, AV Hill Building, Oxford Road, Manchester, M13 9PT UK.
出版信息
Med Chem Res. 2018;27(3):884-889. doi: 10.1007/s00044-017-2110-8. Epub 2017 Nov 13.
Dehydroacetic acid is a common pyrone derivative used commercially as an antibacterial and antifungal agent. Based on the synthesis of dehydroacetic acid () from -hydroxysuccinimdyl acetoacetate, a novel series of enamine-based derivatives were synthesised in order to improve the antibacterial activity of dehydroacetic acid. The antibacterial activities of the synthesised analogues were evaluated against and . Derivative (N-Ph) was identified as the most potent inhibitor of growth. Overall, derivative (N-Me) showed the best broad-spectrum activity with five-fold greater minimum inhibitory concentration and 11-fold greater minimum biocidal concentration against when compared to dehydroacetic acid, in addition to improved antibacterial activity against .
脱氢乙酸是一种常见的吡喃酮衍生物，在商业上用作抗菌和抗真菌剂。基于由乙酰乙酸 - 羟基琥珀酰亚胺酯合成脱氢乙酸（），合成了一系列新型的基于烯胺的衍生物，以提高脱氢乙酸的抗菌活性。对合成的类似物针对 和 的抗菌活性进行了评估。衍生物（N-Ph）被确定为对 生长最有效的抑制剂。总体而言，与脱氢乙酸相比，衍生物（N-Me）表现出最佳的广谱活性，对 的最低抑菌浓度高五倍，最低杀菌浓度高11倍，此外对 的抗菌活性也有所提高。
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