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1-Chloro-2-formyl indenes and tetralenes as antitubercular agents
Authors:Chanda Debabrata  Saikia Dharmendra  Kumar J K  Thakur Jay Prakash  Agarwal Jyoti  Chanotiya C S  Shanker Karuna  Negi Arvind S
Affiliation:a Chemical Sciences Division, Central Institute of Medicinal and Aromatic Plants (CIMAP-CSIR), P.O. CIMAP, Kukrail Picnic Spot Road, Lucknow 226015, U.P., India
b Biotechnology Division, Central Institute of Medicinal and Aromatic Plants (CIMAP-CSIR), P.O. CIMAP, Kukrail, Picnic Spot Road, Lucknow 226015, U.P., India
c CIMAP Research Centre, Hyderabad, A.P., India
Abstract: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.
Keywords:Tetralene   Indene   Antitubercular   Vilsmeier-Haack-Arnold reaction   Acute oral toxicity
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