Bromomethylthioindole Inspired Carbazole Hybrids as Promising Class of Anti-MRSA Agents
| Autor: | I-Wen Huang, Ching-Fang Yeh, De-Jiun Tsai, Chen-Tso Tseng, Yi-Yu Ke, Amit A. Sadani, Kak-Shan Shia, Chun-Ping Chang, Chia-Yi Cheng, Teng-Kuang Yeh, Chien-Huang Wu, Yu-Wei Liu, Guann-Yi Yu, Jinq-Chyi Lee, Yi-Ping Kuo, Jen-Shin Song, Tsai-Ling Lauderdale, Yi-Wun Jhang, Lun K. Tsou |
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| Jazyk: | angličtina |
| Rok vydání: | 2016 |
| Předmět: |
0301 basic medicine
030106 microbiology Biology medicine.disease_cause Biochemistry Enterococcus faecalis Microbiology 03 medical and health sciences chemistry.chemical_compound 0302 clinical medicine Drug Discovery medicine 030212 general & internal medicine Indole test Strain (chemistry) Carbazole Organic Chemistry biochemical phenomena metabolism and nutrition bacterial infections and mycoses biology.organism_classification Methicillin-resistant Staphylococcus aureus In vitro chemistry Staphylococcus aureus Vancomycin medicine.drug |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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