4-Aminoquinoline-chalcone/-N-acetylpyrazoline conjugates: Synthesis and antiplasmodial evaluation

Eur J Med Chem. 2017 Sep 29:138:993-1001. doi: 10.1016/j.ejmech.2017.07.041.

Sumit Kumar ¹, Anu Saini ¹, Jiri Gut ², Philip J Rosenthal ², Raghu Raj ³, Vipan Kumar ⁴

Affiliations

1 Department of Chemistry, Guru Nanak Dev University, Amritsar, 143005, India.
2 Department of Medicine, University of California, San Francisco, CA, USA.
3 Department of Chemistry, DAV College, Amritsar, 143001, India. Electronic address: raghusharma4@gmail.com.
4 Department of Chemistry, Guru Nanak Dev University, Amritsar, 143005, India. Electronic address: vipan_org@yahoo.com.

PMID: 28756265 DOI: 10.1016/j.ejmech.2017.07.041

Abstract

1H-1,2,3-triazole linked 4-aminoquinoline-chalcone/-N-acetylpyrazoline conjugates were synthesized and evaluated against cultured chloroquine (CQ) resistant strain. Antiplasmodial activities of the synthesized conjugates revealed dependence of activity on the length of the alkyl chain as well as on the presence of methoxy substituents on ring A/ring B of the chalcone. The most potent and non-cytotoxic conjugate showed comparable antiplasmodial activity with that of CQ, with an IC₅₀ value of 53.7 nM.

Keywords

4-Aminoquinoline; Antiplasmodial; Chalcone; Click chemistry; N-acetylpyrazoline.

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