Design,synthesis, characterization,antimicrobial evaluation and molecular modeling studies of some dehydroacetic acid-chalcone-1,2,3-triazole hybrids |
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| Institution: | 1. Department of Chemistry, Guru Jambheshwar University of Science and Technology, Hisar, Haryana 125001, India;2. Department of Pharmaceutical Sciences, Guru Jambheshwar University of Science and Technology, Hisar, Haryana 125001, India;3. Department of Bio and Nanotechnology, Guru Jambheshwar University of Science and Technology, Hisar, Haryana 125001, India;4. Department of Chemistry, National Institute of Technology, Kurukshetra, Haryana 136119, India;1. UGC Sponsored Centre for Advanced Studies, Department of Chemistry, Guru Nanak Dev University, Amritsar, 143005, India;2. Department of Pharmacy, Birla Institute of Technology and Science, Pilani Campus, Vidya Vihar, Pilani, 333031, India;3. Department of Microbiology, Guru Nanak Dev University, Amritsar, 143005, India;1. Chemistry Institute, Fluminense Federal University, Outeiro de S. João Batista s/n, Centro, 24020-141 Niterói, RJ, Brazil;2. Department of Pharmaceutical Technology, Faculty of Pharmacy, Fluminense Federal University, Niterói, RJ, Brazil;3. Department of Chemistry, Espírito Santo Federal University, Av. Fernando Ferrari 514, Goiabeiras, 29075-910 Vitória, ES, Brazil;4. Department of Chemistry, Rio de Janeiro Rural Federal University, Seropédica, RJ, Brazil;5. Laboratory of Technological Innovation in Drugs and Cosmetics Development, State University of Maringá, Maringá, PR, Brazil;6. Department of Medicine, University Center of Maringá, Maringá, PR, Brazil |
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| Abstract: | A series of new dehydroacetic acid chalcone-1,2,3-triazole hybrids as potential antimicrobial agents was designed, synthesized and characterized by FTIR, NMR and HRMS spectral techniques. All the synthesized compounds were screened in vitro against four bacterial strains (Staphylococcus epidermidis, Bacillus subtilis, Escherichia coli and Pseudomonas aeruginosa) and two fungal strains (Aspergillus niger and Candida albicans). The antimicrobial results indicated that some of the compounds showed remarkable activities comparable to the standard drugs. Most of the compounds exhibited better efficacy compared to the DHA, which is itself an antimicrobial agent. The synergistic effect in biological activity was observed when DHA, chalcone and 1,2,3-triazole are conjugated. The molecular modeling studies of compound 5j into E. coli topoisomerase II DNA gyrase B were also performed. |
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| Keywords: | Dehydroacetic acid Chalcone 1 2 3-triazole Molecular hybridization Antimicrobial activity |
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