当前位置：
X-MOL 学术
›
ACS Med. Chem. Lett.
›
论文详情
Our official English website, www.x-mol.net, welcomes your
feedback! (Note: you will need to create a separate account there.)
Novel Naphthalimide Aminothiazoles as Potential Multitargeting Antimicrobial Agents
ACS Medicinal Chemistry Letters ( IF 3.5 ) Pub Date : 2017-12-07 00:00:00 , DOI: 10.1021/acsmedchemlett.7b00452 Ying-Ying Chen 1 , Lavanya Gopala 1 , Rammohan R. Yadav Bheemanaboina 1 , Han-Bo Liu 1 , Yu Cheng 1 , Rong-Xia Geng 1 , Cheng-He Zhou 1
ACS Medicinal Chemistry Letters ( IF 3.5 ) Pub Date : 2017-12-07 00:00:00 , DOI: 10.1021/acsmedchemlett.7b00452 Ying-Ying Chen 1 , Lavanya Gopala 1 , Rammohan R. Yadav Bheemanaboina 1 , Han-Bo Liu 1 , Yu Cheng 1 , Rong-Xia Geng 1 , Cheng-He Zhou 1
Affiliation
|
A series of novel naphthalimide aminothiazoles were developed for the first time and evaluated for their antimicrobial activity. Some prepared compounds possessed good inhibitory activity against the tested bacteria and fungi. Noticeably, the piperazine derivative 4d displayed superior antibacterial activity against MRSA and Escherichia coli with MIC values of 4 and 8 μg/mL, respectively, to reference drugs. The most active compound 4d showed low toxicity against mammalian cells with no obvious triggering of the development of bacterial resistance, and it also possessed rapid bactericidal efficacy and efficient membrane permeability. Preliminarily investigations revealed that compound 4d could not only bind with gyrase–DNA complex through hydrogen bonds but could effectively intercalate into MRSA DNA to form 4d–DNA supramolecular complex, which might be responsible for the powerful bioactivity. Further transportation behavior evaluation indicated that molecule 4d could be effectively stored and carried by human serum albumin, and the hydrophobic interactions and hydrogen bonds played important roles in the binding process.
中文翻译：
新型萘二甲酰亚胺咪唑类作为潜在的多靶点抗菌药物
首次开发了一系列新型的萘二甲酰亚胺氨基噻唑，并对其抗菌活性进行了评估。一些制备的化合物对被测细菌和真菌具有良好的抑制活性。值得注意的是，哌嗪衍生物4d对MRSA和大肠杆菌显示出优异的抗菌活性，相对于参考药物的MIC值分别为4和8μg/ mL。活性最高的化合物4d对哺乳动物细胞毒性低，没有明显触发细菌抗性的产生，并且还具有快速的杀菌功效和有效的膜通透性。初步调查显示，化合物4d不仅可以通过氢键与回旋酶-DNA复合物结合，而且可以有效地插入MRSA DNA中以形成4d- DNA超分子复合物，这可能是其强大的生物活性的原因。进一步的运输行为评估表明，分子4d可以被人血清白蛋白有效地存储和携带，疏水相互作用和氢键在结合过程中起着重要作用。
更新日期：2017-12-07
中文翻译：
新型萘二甲酰亚胺咪唑类作为潜在的多靶点抗菌药物
首次开发了一系列新型的萘二甲酰亚胺氨基噻唑，并对其抗菌活性进行了评估。一些制备的化合物对被测细菌和真菌具有良好的抑制活性。值得注意的是，哌嗪衍生物4d对MRSA和大肠杆菌显示出优异的抗菌活性，相对于参考药物的MIC值分别为4和8μg/ mL。活性最高的化合物4d对哺乳动物细胞毒性低，没有明显触发细菌抗性的产生，并且还具有快速的杀菌功效和有效的膜通透性。初步调查显示，化合物4d不仅可以通过氢键与回旋酶-DNA复合物结合，而且可以有效地插入MRSA DNA中以形成4d- DNA超分子复合物，这可能是其强大的生物活性的原因。进一步的运输行为评估表明，分子4d可以被人血清白蛋白有效地存储和携带，疏水相互作用和氢键在结合过程中起着重要作用。
京公网安备 11010802027423号