Design,synthesis and antiplasmodial activity of novel imidazole derivatives based on 7-chloro-4-aminoquinoline |
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| Affiliation: | 1. Medicinal & Process Chemistry Division, CSIR-Central Drug Research Institute Sector-10, Jankipuram Extension, Sitapur Road, Lucknow 226031, India;2. Parasitology Division, CSIR-Central Drug Research Institute, Sector-10, Jankipuram Extension, Sitapur Road, Lucknow 226031, India;1. H. E. J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi 75270, Pakistan;2. Department of Pharmaceutical Sciences, Faculty of Pharmacy and Medical Sciences, Al-Ahliyya Amman University, Amman 19328, Jordan;3. Department of Chemistry, Faculty of Science, The University of Jordan, Amman 11942, Jordan;4. Department of Physical Sciences, Faculty of Applied Sciences, South Eastern University, Oluvil, Sri Lanka;5. Department of Biochemistry, Faculty of Science, King Abdulaziz University, Jeddah-21412, Saudi Arabia;1. Normandie Univ, UNIROUEN, COBRA, INSA Rouen, CNRS, COBRA, 76000 Rouen, France;2. Normandie Univ, UNIROUEN, SMS EA3233, 76000 Rouen, France;1. Department of Chemistry, Sardar Patel University, Vallabh Vidyanagar, 388120, Gujarat, India;2. Department of Chemistry, Marwadi University, Rajkot, Gujarat, India |
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| Abstract: | A series of short chain 4-aminoquinoline-imidazole derivatives have been synthesized in one pot two step multicomponent reaction using van leusen standard protocol. The diethylamine function of chloroquine is replaced by substituted imidazole derivatives containing tertiary terminal nitrogen. All the synthesized compounds were screened against the chloroquine sensitive (3D7) and chloroquine resistant (K1) strains of Plasmodium falciparum. Some of the compounds (6, 8, 9 and 17) in the series exhibited comparable activity to CQ against K1 strain of P. falciparum. All the compounds displayed resistance factor between 0.09 and 4.57 as against 51 for CQ. Further, these analogues were found to form a strong complex with hematin and inhibit the β-hematin formation, therefore these compounds act via heme polymerization target. |
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| Keywords: | 4-Aminoquinoline Antiplasmodial activity Heme binding Chloroquine Chloroquine sensitive strain Chloroquine resistant strain CQ" },{" #name" :" keyword" ," $" :{" id" :" k0055" }," $$" :[{" #name" :" text" ," _" :" chloroquine DMF" },{" #name" :" keyword" ," $" :{" id" :" k0065" }," $$" :[{" #name" :" text" ," _" :" dimethylformamide TOSMIC" },{" #name" :" keyword" ," $" :{" id" :" k0075" }," $$" :[{" #name" :" text" ," _" :" Toluenesulfonylmethyl isocyanide |
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