2. Academic Validation
  3. Synthesis of 4-aminoquinoline-pyrimidine hybrids as potent antimalarials and their mode of action studies

Synthesis of 4-aminoquinoline-pyrimidine hybrids as potent antimalarials and their mode of action studies

  • Eur J Med Chem. 2013 Aug:66:314-23. doi: 10.1016/j.ejmech.2013.05.046.
Kamaljit Singh 1,  Hardeep Kaur,  Kelly Chibale,  Jan Balzarini
Affiliations

Affiliation

  • 1 Department of Chemistry, UGC-Centre of Advance Study-1, Guru Nanak Dev University, Amritsar, Punjab 143005, India. kamaljit19in@yahoo.co.in
PMID: 23811093 DOI: 10.1016/j.ejmech.2013.05.046
Abstract

One of the most viable options to tackle the growing resistance to the antimalarial drugs such as artemisinin is to resort to synthetic drugs. The multi-target strategy involving the use of hybrid drugs has shown promise. In line with this, new hybrids of quinoline with pyrimidine have been synthesized and evaluated for their antiplasmodial activity against both CQ(S) and CQ(R) strains of Plasmodium falciparum. These depicted activity in nanomolar range and were found to bind to heme as well as AT rich pUC18 DNA.

Keywords

4-Aminoquinolines; Antimalarials; Drug discovery; Heme binding; Hybrid molecules.

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