当前位置: X-MOL 学术Chem. Pharm. Bull. › 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.)
Structure–Activity Relationship Studies of Antimicrobial Naphthoquinones Derived from Constituents of Tabebuia avellanedae
Chemical & Pharmaceutical Bulletin ( IF 1.5 ) Pub Date : 2021-07-01 , DOI: 10.1248/cpb.c21-00208
Mitsuaki Yamashita 1 , Jun Sawano 1 , Ryuji Umeda 1 , Ayuka Tatsumi 1 , Yuko Kumeda 2 , Akira Iida 1
Affiliation  

In this study, based on our previous study, derivatives of naphtho[2,3-b]furan-4,9-diones were synthesized and their antimicrobial activities were evaluated. The screening of these naphthoquinones revealed that the fluorine-containing NQ008 compound exhibited potent and broad antimicrobial activities against Gram-positive bacteria including methicillin-resistant Staphylococcus aureus (MRSA), Gram-negative bacteria, and fungi. The results of the ratio of the minimum bactericidal concentration (MBC) to the minimum inhibitory concentrations (MICs) and time–kill assays suggest that the mode of action of NQ008 is bactericidal. Additionally, the results of a drug resistance study revealed that NQ008 exhibited potent antibacterial activity and may delay the development of bacteria resistance. Furthermore, NQ008 exhibited preliminary antiviral activity against the swine influenza virus and Feline calicivirus.

Fullsize Image


中文翻译:

来自Tabebuia avellanedae 成分的抗菌萘醌的构效关系研究

在本研究中,基于我们之前的研究,合成了萘并[2,3 - b ]呋喃-4,9-二酮的衍生物并评估了它们的抗菌活性。对这些萘醌化合物的筛选表明,含氟NQ008化合物对革兰氏阳性菌(包括耐甲氧西林金黄色葡萄球菌(MRSA)、革兰氏阴性菌和真菌)表现出强大而广泛的抗菌活性。最低杀菌浓度 (MBC) 与最低抑菌浓度 (MIC) 之比和时间-杀灭试验结果表明NQ008的作用方式是杀菌。此外,一项耐药性研究的结果表明,NQ008表现出有效的抗菌活性,并可能延缓细菌耐药性的发展。此外,NQ008对猪流感病毒和猫杯状病毒表现出初步的抗病毒活性。

全尺寸图像
更新日期:2021-06-30
down
wechat
bug