Synthesis of novel thiourea,thiazolidinedione and thioparabanic acid derivatives of 4-aminoquinoline as potent antimalarials |
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| Authors: | Naresh Sunduru Kumkum Srivastava S Rajakumar SK Puri JK Saxena Prem MS Chauhan |
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| Institution: | 1. Division of Medicinal and Process Chemistry, Central Drug Research Institute, Lucknow 226 001, India;2. Division of Parasitology, Central Drug Research Institute, Lucknow 226 001, India;3. Division of Biochemistry, Central Drug Research Institute, Lucknow 226 001, India |
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| Abstract: | In search of new 4-aminoquinolines which are not recognized by CQR mechanism, thiourea, thiazolidinedione and thioparabanic acid derivatives of 4-aminoquinoline were synthesized and screened for their antimalarial activities. Thiourea derivative 3 found to be the most active against CQ sensitive strain 3D7 of Plasmodium falciparum in an in vitro model with an IC50 of 6.07 ng/mL and also showed an in vivo suppression of 99.27% on day 4 against CQ resistant strain N-67 of Plasmodium yoelii. |
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