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Design, synthesis and antiplasmodial activity of novel imidazole derivatives based on 7-chloro-4-aminoquinoline

Publication date:

October 2018


Source:Bioorganic Chemistry, Volume 80

Author(s): Srinivasarao Kondaparla, Ashan Manhas, Vasantha Rao Dola, Kumkum Srivastava, Sunil K. Puri, S.B. Katti

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.
Graphical abstract




Authors:   Author(s): Srinivasarao Kondaparla, Ashan Manhas, Vasantha Rao Dola, Kumkum Srivastava, Sunil K. Puri, S.B. Katti
Journal:   Bioorganic Chemistry
Volume:   80
Year:   2018
Pages:   204
DOI:   10.1016/j.bioorg.2018.06.012
Publication date:   25-Jun-2018
Facts, background information, dossiers
  • imidazole
  • chloroquine
  • Plasmodium falciparum
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