Synthesis,antimalarial properties and 2D-QSAR studies of novel triazole-quinine conjugates |
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| Institution: | 1. Department of Chemistry, Faculty of Science, King Abdulaziz University, Jeddah, Saudi Arabia;2. Department of Chemistry & Physics, Augusta University, Augusta, GA 30912, USA;3. Center for Heterocyclic Compounds, Department of Chemistry, University of Florida, Gainesville, FL 32611-7200, USA;4. Pesticide Chemistry Department, National Research Centre, Dokki, Giza 12622, Egypt;5. Center for World Health & Medicine, Saint Louis University, Saint Louis, MO 63104, USA;1. Department of Chemistry, MMV, Banaras Hindu University (B.H.U), Varanasi, 221005, India;2. Department of Physics, MMV, Banaras Hindu University (B.H.U), Varanasi, 221005, India;3. Institute of Medical Science, Banaras Hindu University (B.H.U), Varanasi, 221005, India;1. Drug Discovery and Development Research Group, College of Pharmacy and Nutrition, University of Saskatchewan, Saskatoon, Saskatchewan S7N 5C9, Canada;2. Division of Experimental Therapeutics, Walter Reed Army Institute of Research, Silver Spring, MD 20910, USA;1. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Egyptian Russian University, Badr City, Cairo, P.O. Box 11829, Egypt;2. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Suez Canal University, Ismailia, P.O. Box 41522, Egypt;3. The Regional Center for Mycology and Biotechnology, Al-Azhar University, Cairo, Egypt;4. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Al-Azhar University, Cairo, P.O. Box 11471, Egypt;1. Key Laboratory for Organic Electronics and Information Displays & Institute of Advanced Materials (IAM), Jiangsu National Synergetic Innovation Center for Advanced Materials (SICAM), Nanjing University of Posts & Telecommunications, 9 Wenyuan Road, Nanjing 210023, China;2. School of Geography and Biological Information, Nanjing University of Posts & Telecommunications, 9 Wenyuan Road, Nanjing 210023, China |
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| Abstract: | Click chemistry technique led to novel 1,2,3-triazole-quinine conjugates 8a–g, 10a–o, 11a–h and 13 utilizing benzotriazole-mediated synthetic approach with excellent yields. Some of the synthesized analogs (11a, 11d–h) exhibited antimalarial properties against Plasmodium falciparum strain 3D7 with potency higher than that of quinine (standard reference used) through in vitro standard procedure bio-assay. Statistically significant BMLR-QSAR model describes the bio-properties, validates the observed biological observations and identifies the most important parameters governing bio-activity. |
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| Keywords: | Antimalarial Quinine Triazole Click chemistry QSAR |
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