Multicomponent Petasis‐borono Mannich Preparation of Alkylaminophenols and Antimicrobial Activity Studies |
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| Authors: | Íris Neto Joana Andrade Prof. A. S. Fernandes Catarina Pinto Reis Jagadish K. Salunke Prof. Arri Priimagi Prof. Nuno R. Candeias Prof. Patrícia Rijo |
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| Affiliation: | 1. Center for Research in Biosciences & Health Technologies (CBIOS), Universidade Lusófona de Humanidades e Tecnologias, Lisboa, Portugal;2. Department of Chemistry and Bioengineering, Tampere University of Technology, Tampere, Finland;3. Instituto de Investiga??o do Medicamento (iMed.ULisboa), Faculdade de Farmácia, Universidade de Lisboa, Lisboa, Portugal |
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| Abstract: | In this work we report the antibacterial activity of alkylaminophenols. A series of such compounds was prepared by a multicomponent Petasis‐borono Mannich reaction starting from salicylaldehyde and its derivatives. The obtained compounds were tested against a large panel of microorganisms, Gram‐positive and Gram‐negative bacteria, and a yeast. Among the several tertiary amine derivatives tested, indoline‐derived aminophenols containing a nitro group at the para‐phenol position showed considerable activity against bacteria tested with minimal inhibitory concentrations as low as 1.36 μm against Staphyloccocus aureus and Mycobacterium smegmatis. Cytotoxicity of the new para‐nitrophenol derivatives was observed only at concentrations much higher than those required for antibacterial activity. |
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| Keywords: | alkylaminophenols antibacterial activity multicomponent reactions structure– activity relationships |
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