Synthesis and evaluation of new diaryl ether and quinoline hybrids as potential antiplasmodial and antimicrobial agents |
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| Affiliation: | 1. Medicinal and Process Chemistry Division, CSIR-Central Drug Research Institute, BS-10/1, Sector 10, Jankipuram Extension, Sitapur Road, Lucknow 226031, Uttar Pradesh, India;2. Parasitology Division, CSIR-Central Drug Research Institute, BS-10/1, Sector 10, Jankipuram Extension, Sitapur Road, Lucknow 226031, Uttar Pradesh, India;3. Microbiology Division, CSIR-Central Drug Research Institute, BS-10/1, Sector 10, Jankipuram Extension, Sitapur Road, Lucknow 226031, Uttar Pradesh, India;4. Academy of Scientific and Innovative Research, New Delhi, India;1. Department of Biochemistry and Molecular Biology, Bio21 Molecular Science and Biotechnology Institute, The University of Melbourne, Vic. 3010, Australia;2. Australian Research Council Centre of Excellence for Coherent X-ray Science, Australia;3. Department of Physics, La Trobe University, Vic. 3071, Australia;4. Electron Microscopy Unit, Bio21 Molecular Science and Biotechnology Institute, The University of Melbourne, Melbourne, Vic. 3010, Australia;5. Department of Computer Science and Software Engineering, The University of Melbourne, Vic. 3010, Australia;1. Department of Chemistry, School of Arts and Sciences, The Johns Hopkins University, 3400 North Charles Street, Baltimore, MD 21218, United States;2. W. Harry Feinstone Department of Molecular Microbiology and Immunology, Bloomberg School of Public Health, The Johns Hopkins University, Baltimore, MD 21205, United States;3. The Johns Hopkins Malaria Research Institute, Bloomberg School of Public Health, The Johns Hopkins University, Baltimore, MD 21205, United States;1. Departamento de Biofísica, Universidade Federal de São Paulo, Rua Pedro de Toledo, 699, 7° andar, 04039-032 São Paulo, Brazil;2. Departamento de Microbiologia, Imunologia e Parasitologia, Universidade Federal de São Paulo, Rua Botucatu, 862, 8° andar, 04023-062 São Paulo, SP, Brazil;3. Departamento de Biociências, Universidade Federal de São Paulo, Avenida Ana Costa, 95, 11060-001 Santos, SP, Brazil;1. Université de Rennes 1, Institut des Sciences Chimiques de Rennes, CNRS UMR 6226, Avenue du Général Leclerc, 35042 Rennes Cedex, France;2. UMR 892 INSERM/6299 CNRS/Université de Nantes, Team 8 “Cell survival and tumor escape in breast cancer”, Institut de Recherche Thérapeutique de l’Université de Nantes, 8 quai Moncousu, BP 70721, 44007 Nantes Cedex 1, France;3. Institut de Cancérologie de l’Ouest, Centre de Lutte contre le Cancer René Gauducheau, Boulevard Jacques Monod, 44805 Saint Herblain-Nantes Cedex, France;4. Plateforme IMPACT®, Biogenouest Institut de Recherche Thérapeutique de l’Université de Nantes, 8 quai Moncousu, BP 70721, 44007 Nantes Cedex 1, France;5. Bioprojet-Biotech, 4 rue du Chesnay Beauregard, BP 96205, 35762 Saint Grégoire, France |
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| Abstract: | Synthesis and bioevaluation of new diaryl ether hybridized quinoline derivatives as antiplasmodial, antibacterial and antifungal agents is reported. It was encouraging to discover that several compounds displayed 2–3 folds better efficacy than chloroquine in chloroquine-resistant K1 strain of Plasmodium falciparum. Further, a few members of the library displayed good antibacterial efficacy against gram positive strains of bacteria but none of the compounds displayed any significant antifungal activity. |
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| Keywords: | Diaryl ether Quinoline Hybrid Malaria Antibacterial |
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