Synthesis and biological evaluation of 8-substituted berberine derivatives as novel anti-mycobacterial agents
Tuberculosis (TB) is a disease which kills two million people every year and infects over one-third of the world′s population. Eighteen new 8-substituted berberine derivatives were synthesized and evaluated for their anti-mycobacterial activities against Mycobacterium tuberculosis (M. tuberculosis)...
| Main Authors: | , , , , |
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| Format: | Article |
| Language: | English |
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Elsevier
2012-12-01
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| Series: | Acta Pharmaceutica Sinica B |
| Subjects: | |
| Online Access: | http://www.sciencedirect.com/science/article/pii/S2211383512001475 |
| _version_ | 1811235497354199040 |
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| author | Yanxiang Wang Haigen Fu Yinghong Li Jiandong Jiang Danqing Song |
| author_facet | Yanxiang Wang Haigen Fu Yinghong Li Jiandong Jiang Danqing Song |
| author_sort | Yanxiang Wang |
| collection | DOAJ |
| description | Tuberculosis (TB) is a disease which kills two million people every year and infects over one-third of the world′s population. Eighteen new 8-substituted berberine derivatives were synthesized and evaluated for their anti-mycobacterial activities against Mycobacterium tuberculosis (M. tuberculosis) strain H37Rv. Among these compounds, compound 6i was the most effective antitubercular agent with an MIC of 1.0 μg/mL. Most importantly, compound 6i also exhibited a potent effect against clinically isolated rifampicin- and isoniazid-resistant M. tuberculosis strains, suggesting a different mode of action from the current drugs. Therefore, it shows potential for the development of new anti-TB agents. |
| first_indexed | 2024-04-12T11:52:51Z |
| format | Article |
| id | doaj.art-b6e5b330edfd454097493f69b7459878 |
| institution | Directory Open Access Journal |
| issn | 2211-3835 2211-3843 |
| language | English |
| last_indexed | 2024-04-12T11:52:51Z |
| publishDate | 2012-12-01 |
| publisher | Elsevier |
| record_format | Article |
| series | Acta Pharmaceutica Sinica B |
| spelling | doaj.art-b6e5b330edfd454097493f69b74598782022-12-22T03:34:08ZengElsevierActa Pharmaceutica Sinica B2211-38352211-38432012-12-012658158710.1016/j.apsb.2012.10.008Synthesis and biological evaluation of 8-substituted berberine derivatives as novel anti-mycobacterial agentsYanxiang WangHaigen FuYinghong LiJiandong JiangDanqing SongTuberculosis (TB) is a disease which kills two million people every year and infects over one-third of the world′s population. Eighteen new 8-substituted berberine derivatives were synthesized and evaluated for their anti-mycobacterial activities against Mycobacterium tuberculosis (M. tuberculosis) strain H37Rv. Among these compounds, compound 6i was the most effective antitubercular agent with an MIC of 1.0 μg/mL. Most importantly, compound 6i also exhibited a potent effect against clinically isolated rifampicin- and isoniazid-resistant M. tuberculosis strains, suggesting a different mode of action from the current drugs. Therefore, it shows potential for the development of new anti-TB agents.http://www.sciencedirect.com/science/article/pii/S2211383512001475BerberineAnti-tubercularStructure-activity relationshipDrug-resistanceH37Rv |
| spellingShingle | Yanxiang Wang Haigen Fu Yinghong Li Jiandong Jiang Danqing Song Synthesis and biological evaluation of 8-substituted berberine derivatives as novel anti-mycobacterial agents Acta Pharmaceutica Sinica B Berberine Anti-tubercular Structure-activity relationship Drug-resistance H37Rv |
| title | Synthesis and biological evaluation of 8-substituted berberine derivatives as novel anti-mycobacterial agents |
| title_full | Synthesis and biological evaluation of 8-substituted berberine derivatives as novel anti-mycobacterial agents |
| title_fullStr | Synthesis and biological evaluation of 8-substituted berberine derivatives as novel anti-mycobacterial agents |
| title_full_unstemmed | Synthesis and biological evaluation of 8-substituted berberine derivatives as novel anti-mycobacterial agents |
| title_short | Synthesis and biological evaluation of 8-substituted berberine derivatives as novel anti-mycobacterial agents |
| title_sort | synthesis and biological evaluation of 8 substituted berberine derivatives as novel anti mycobacterial agents |
| topic | Berberine Anti-tubercular Structure-activity relationship Drug-resistance H37Rv |
| url | http://www.sciencedirect.com/science/article/pii/S2211383512001475 |
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