1,2,3-Triazole-derived naphthalimides as a novel type of potential antimicrobial agents: Synthesis,antimicrobial activity,interaction with calf thymus DNA and human serum albumin |
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| Affiliation: | 1. Department of Chemistry, GITAM Institute of Sciences, GITAM University, Visakhapatnam, Andhra Pradesh, India;2. School of Chemistry & Physics, University of KwaZulu-Natal, Westville Campus, Chiltern Hills, Durban-4000, South Africa;1. LAQV, REQUIMTE, Departamento de Química, Faculdade de Ciências e Tecnologia, Universidade Nova de Lisboa, 2829-516 Caparica, Portugal;2. Instituto Superior de Ciências da Saúde Egas Moniz, 2829-511 Caparica, Portugal;3. Mountain Research Centre (CIMO), ESA, Polytechnic Institute of Bragança, Campus de Santa Apolónia, 1172, 5301-855 Bragança, Portugal;4. Department of Plant Physiology, Institute for Biological Research, “Siniša Stanković”, University of Belgrade, Bulevar Despota Stefana 142, 11000 Belgrade, Serbia |
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| Abstract: | A series of 1,2,3-triazole-derived naphthalimides as a novel type of potential antimicrobial agents were synthesized and characterized by IR, NMR and HRMS spectra. All the new compounds were screened for their antimicrobial activity against four Gram-positive bacteria, four Gram-negative bacteria and three fungi. Bioactive assay manifested that 3,4-dichlorobenzyl compound 9e and its corresponding hydrochloride 11e showed better anti-Escherichia coli activity than Norfloxacin and Chloromycin. Preliminary research revealed that compound 9e could effectively intercalate into calf thymus DNA to form compound 9e–DNA complex which might block DNA replication and thus exert antimicrobial activities. Human serum albumin could effectively store and carry compound 9e by electrostatic interaction. |
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| Keywords: | Antibacterial Triazole Human serum albumin Naphthalimide DNA |
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