國家衛生研究院 NHRI:Item 3990099045/10129
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    题名: Bromomethylthioindole inspired carbazole hybrids as promising class of anti-MRSA agents
    作者: Cheng, CY;Chang, CP;Yang, LTL;Yu, GY;Lee, JC;Jhang, YW;Wu, CH;Ke, YY;Sadani, AA;Yeh, CF
    贡献者: Institute of Biotechnology and Pharmaceutical Research;Division of Infectious Diseases
    摘要: Series of N-substituted carbazole analogues bearing an indole ring were synthesized as anti-methicillin-resistant Staphylococcus aureus (MRSA) agents from a molecular hybridization approach. The representative compound 19 showed an MIC = 1 μg/mL against a panel of MRSA clinical isolates as it possessed comparable in vitro activities to that of vancomycin. Moreover, compound 19 also exhibited MIC = 1 μg/mL activities against a recent identified Z172 MRSA strain (vancomycin-intermediate and daptomycin-nonsusceptible phenotype) and the vancomycin-resistant Enterococcus faecalis (VRE) strain. In a mouse model with lethal infection of MRSA (4N216), a 75% survival rate was observed after a single dose of compound 19 was intravenously administered at 20 mg/kg. In light of their equipotent activities against different MRSA isolates and VRE strain, the data underscore the importance of designed hybrid series for the development of new N-substituted carbazoles as potential anti-MRSA agents.
    日期: 2016-12-08
    關聯: ACS Medicinal Chemistry Letters. 2016 Dec 8;7(12):1191-1196.
    Link to: http://dx.doi.org/10.1021/acsmedchemlett.6b00289
    JIF/Ranking 2023: http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=NHRI&SrcApp=NHRI_IR&KeyISSN=1948-5875&DestApp=IC2JCR
    Cited Times(WOS): https://www.webofscience.com/wos/woscc/full-record/WOS:000389622100039
    Cited Times(Scopus): http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=85003881281
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