2. Academic Validation
  3. Synthesis of oxalamide and triazine derivatives as a novel class of hybrid 4-aminoquinoline with potent antiplasmodial activity

Synthesis of oxalamide and triazine derivatives as a novel class of hybrid 4-aminoquinoline with potent antiplasmodial activity

  • Bioorg Med Chem. 2009 Sep 1;17(17):6451-62. doi: 10.1016/j.bmc.2009.05.075.
Naresh Sunduru 1,  Moni Sharma,  Kumkum Srivastava,  S Rajakumar,  S K Puri,  J K Saxena,  Prem M S Chauhan
Affiliations

Affiliation

  • 1 Division of Medicinal and Process Chemistry, Central Drug Research Institute, Lucknow 226001, India.
PMID: 19665899 DOI: 10.1016/j.bmc.2009.05.075
Abstract

Frequency of malaria and its resistance to chemotherapeutic options are emerging rapidly. To counter this problem, a series of 4-aminoquinolines having oxalamide and triazine functionalities in the side chain were synthesized and screened for their antimalarial activities. Triazine derivative 48 found to be the most active against CQ sensitive strain 3D7 of Plasmodium falciparum in an in vitro assay with an IC(50) of 5.23 ng/mL and oxalamide derivative 13 showed an in vivo suppression of 70.45% on day 4 against CQ resistant strain N-67 of Plasmodium yoelii.

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