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1H-1,2,3-Triazole-tethered isatin-7-chloroquinoline and 3-hydroxy-indole-7-chloroquinoline conjugates: Synthesis and antimalarial evaluation
Affiliation:1. Photochemistry Department, Chemical Industries Research Institute, National Research Centre, 33 El Buhouth Street, P.O. Box 12622, Cairo, Egypt;2. Pesticide Chemistry Department, Chemical Industries Research Institute, National Research Centre, 33 El Buhouth Street, P.O. Box 12622, Cairo, Egypt;3. Water Pollution Research Department, Environmental and Climate Change Research Institute, National Research Centre, 33 El Buhouth Street, P.O. Box 12622, Cairo, Egypt;4. Radioisotopes Department, Nuclear Research Centre, Egyptian Atomic Energy Authority, Cairo, Egypt;5. Pharmacognosy Department, Pharmaceutical and Drug Industries Research Institute, National Research Centre, 33 El Buhouth Street, P.O. Box 12622, Cairo, Egypt
Abstract:A series of 1H-1,2,3-triazole-tethered isatin-7-chloroquinoline and 3-hydroxy-indole-7-chloroquinoline conjugates have been synthesized and evaluated for their antimalarial activity against chloroquine-resistant W2 strain of Plasmodium falciparum. The most potent of the test compound with an optimum combination of 3-hydroxy-indole ring and a n-butyl linker displayed an IC50 value of 69 nM.
Keywords:7-Chloroquinoline  Isatin  3-Hydroxy-indole-2-one  Antimalarial activity
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