Biotechnology Division, Central Institute of Medicinal and Aromatic Plants (CIMAP-CSIR), PO CIMAP, Kukrail, Picnic Spot Road, Lucknow 226015, UP, India.
Bioorg Med Chem Lett. 2011 Jul 1;21(13):3966-9. doi: 10.1016/j.bmcl.2011.05.016. Epub 2011 May 14.
1-Chloro-2-formyl indenes and tetralenes have been synthesized using Vilsmeier-Haack-Arnold reaction onto indanones and tetralones. Most of these analogues exhibited antitubercular activity against Mycobacterium tuberculosis H37Rv strain with MICs ranging from 30 to 500 μg/mL. Analogue 13 was further modified to some derivatives. The most active analogue 23 showing MIC at 30 μg/mL was further evaluated for acute oral toxicity in Swiss albino mice and was found to be safe up to 300 mg/kg dose.
1-氯-2-甲酰基茚满和四氢萘已通过 Vilsmeier-Haack-Arnold 反应在茚满酮和四氢萘酮上合成。大多数这些类似物对结核分枝杆菌 H37Rv 株显示出抗结核活性,MIC 范围为 30 至 500μg/mL。类似物 13 进一步被修饰为一些衍生物。显示 MIC 为 30μg/mL 的最活性类似物 23 进一步在瑞士白化小鼠中进行了急性口服毒性评估,发现其在 300mg/kg 剂量下是安全的。