期刊
MARINE DRUGS
卷 12, 期 4, 页码 1757-1772出版社
MDPI
DOI: 10.3390/md12041757
关键词
synthesis; caulerpin; analogues; anti-tuberculosis activity
资金
- CONACyT (Consejo Nacional de Ciencia y Tecnologia) [131295, 223436]
Caulerpin (1a), a bis-indole alkaloid from the marine algal Caulerpa sp., was synthesized in three reaction steps with an overall yield of 11%. The caulerpin analogues (1b-1g) were prepared using the same synthetic pathway with overall yields between 3% and 8%. The key reaction involved a radical oxidative aromatic substitution involving xanthate (3) and 3-formylindole compounds (4a-4g). All bis-indole compounds synthesized were evaluated against the Mycobacterium tuberculosis strain H37Rv, and 1a was found to display excellent activity (IC50 0.24 mu M).
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