Design,synthesis and antibacterial activity evaluation of moxifloxacin-amide-1,2,3-triazole-isatin hybrids |
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| Affiliation: | 1. State Key Laboratory of Biobased Material and Green Papermaking (LBMP), Qilu University of Technology (Shandong Academy of Sciences), Jinan, PR China;2. Shanghai Key Laboratory of Molecular Imaging, Shanghai University of Medicine and Health Sciences, Shanghai, PR China;1. College of Chemistry, Fuzhou University, Fuzhou, Fujian 350116, China;2. Shanghai Key Laboratory of Green Chemistry and Chemical Processes, Department of Chemistry, School of Chemistry and Molecular Engineering, East China Normal University, Shanghai 200241, China;1. Department of Medical Imaging, Jinling Hospital, Medical School of Nanjing University, Nanjing, PR China;2. Life Sciences, TRIUMF, Vancouver, Canada;3. Department of Neurosurgery, NanJing Drum Tower Hospital, The Affiliated Hospital of Nanjing University Medical School, Nanjing, PR China;1. Wuhan University of Science and Technology, 430081, China;2. Pony Testing International Group, Wuhan 430034, China;3. WuXi AppTec, Wuhan 430075, China;4. Hengshui University, Hengshui 053000, China;5. Synthetic and Functional Biomolecules Center, Peking University, Beijing 100871, China;1. Department of Chemistry, National Institute of Technology, Warangal 506004, Telangana, India;2. Environmental Monitoring &Exposure Assessment (Air) Laboratory, ICMR-NIREH, Bhopal 462 030, MP, India;3. Medicinal Chemistry and Pharmacology Division, CSIR–IICT, Hyderabad 500 007, Telangana, India;4. Division of Microbiology, CSIR−CDRI, Jankipuram Extension, Sitapur Road, Lucknow 226031, UP, India;5. Department of Chemistry, National Institute of Technology, Calicut 673601, Kerala, India;1. Key Laboratory of Hubei Province for Coal Conversion and New Carbon Materials, Wuhan University of Science and Technology, Hubei, PR China;2. Pony Testing International Group (Wuhan), Hubei, PR China;3. Beijing University of Technology, Beijing, PR China;1. State Key Laboratory of Biobased Material and Green Papermaking (LBMP), Qilu University of Technology (Shandong Academy of Sciences), Jinan, PR China;2. Department of Medical Imaging, Jinling Hospital, Medical School of Nanjing University, Nanjing, PR China;3. Shanghai Key Laboratory of Molecular Imaging, Shanghai University of Medicine and Health Sciences, Shanghai, PR China;4. Wuhan University of Science and Technology, Wuhan, Hubei, PR China |
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| Abstract: | In this work, a series of novel moxifloxacin-amide-1,2,3-triazole-isatin hybrids 7a-l were designed and synthesized. The in vitro antibacterial activity against a panel of clinically important Gram-positive and Gram-negative bacteria including drug-resistant pathogens was also evaluated. All hybrids showed considerable activity against the tested pathogens with MIC values of ≤0.03 to 128 μg/mL, and some of them such as hybrids 7e, 7g and 7j were comparable to or better than the parent moxifloxacin (MIC: ≤0.03–8 μg/mL). Moreover, hybrids 7e, 7g and 7j also demonstrated low cytotoxicity towards CHO cells. However, the in vivo pharmacokinetic profiles of these three hybrids were generally far inferior to the parent moxifloxacin. The structure-activity relationship and structure-cytotoxicity relationship were also studied and discussed which may help with the identification of new chemical entities as potent antibacterial agents. |
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| Keywords: | Moxifloxacin Amide Isatin 1,2,3-Triazole Antibacterial Drug-resistant pathogen Structure-activity relationship |
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