1-Chloro-2-formyl indenes and tetralenes as antitubercular agents

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.

Indene and tetralene analogues have been synthesized using Vilsmeier–Haack–Arnold reaction. All these compounds exhibited antimycobacterial activity against H37Rv. Analogue 23, exhibiting antimycobacterial activity (MIC 30 μg/mL) was found to be safe up to 300 mg/kg dose in acute oral toxicity in Swiss albino mice.Figure optionsDownload as PowerPoint slide