Silver triflate catalyzed synthesis of 3-aminoalkylated indoles and evaluation of their antibacterial activities

V. Kameshwara Rao1, M. Sudershan Rao1, N. K. Jain2, Jitendra Panwar2, Anil Kumar1
1Department of Chemistry, Birla Institute of Technology and Science, Pilani 333 031, Rajasthan, India
2Department of Biological Sciences, Birla Institute of Technology and Science, Pilani 333 031, Rajasthan, India

Tóm tắt

Abstract An efficient, one-pot synthesis was developed for 3-aminoalkylated indoles by three-component coupling reaction of aldehydes, N-methylanilines, and indoles using AgOTf as a catalyst. A series of twenty 3-aminoalkylated indoles was evaluated for their antibacterial activities against both Gram negative and Gram positive bacteria. Compounds 4b and 4r showed good antibacterial activity against both Gram positive and Gram negative strains. However, inversing the property of substituent (from 4r to 4q) resulted in the significant fall in the magnitude of antibacterial activity against Escherichia coli.

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