Literature DB >> 28332319

Piperazine-linked 4-aminoquinoline-chalcone/ferrocenyl-chalcone conjugates: Synthesis and antiplasmodial evaluation.

Amandeep Singh1, Anu Rani1, Jiri Gut2, Philip J Rosenthal2, Vipan Kumar1.   

Abstract

A series of piperazine-linked 4-aminoquinoline-chalcone/ferrocenyl-chalcone conjugates were prepared with a view to evaluate their activities against Plasmodium falciparum. The synthesized conjugates had in vitro IC50 values from 0.41 to 2.38 μm against chloroquine-resistant and mefloquine-sensitive W2 strain of P. falciparum. The submicromolar activities of most of the synthesized conjugates suggest that such molecular frameworks can act as therapeutic templates for the design and synthesis of new antimalarials.
© 2017 John Wiley & Sons A/S.

Entities:  

Keywords:  4-aminoquinoline-ferrocenyl-chalcone; aldol condensation; antiplasmodial activities; structure-activity relationship

Mesh:

Substances:

Year:  2017        PMID: 28332319     DOI: 10.1111/cbdd.12982

Source DB:  PubMed          Journal:  Chem Biol Drug Des        ISSN: 1747-0277            Impact factor:   2.817


  4 in total

1.  Chalcones as a basis for computer-aided drug design: innovative approaches to tackle malaria.

Authors:  Marilia Nn Lima; Bruno J Neves; Gustavo C Cassiano; Marcelo N Gomes; Kaira Cp Tomaz; Leticia T Ferreira; Tatyana A Tavella; Juliana Calit; Daniel Y Bargieri; Eugene N Muratov; Fabio Tm Costa; Carolina Horta Andrade
Journal:  Future Med Chem       Date:  2019-09-26       Impact factor: 3.808

2.  Design, synthesis, heme binding and density functional theory studies of isoindoline-dione-4-aminoquinolines as potential antiplasmodials.

Authors:  Anu Rani; Sumit Kumar; Jenny Legac; Adebayo A Adeniyi; Paul Awolade; Parvesh Singh; Philip J Rosenthal; Vipan Kumar
Journal:  Future Med Chem       Date:  2019-12-05       Impact factor: 3.808

Review 3.  Two Important Anticancer Mechanisms of Natural and Synthetic Chalcones.

Authors:  Teodora Constantinescu; Alin Grig Mihis
Journal:  Int J Mol Sci       Date:  2022-09-30       Impact factor: 6.208

4.  Design, Synthesis and Preliminary Antimicrobial Evaluation of N-Alkyl Chain Tethered C-5 Functionalized Bis-Isatins.

Authors:  Amandeep Singh; Trpta Bains; Hye Jee Hahn; Nicole Liu; Christina Tam; Luisa W Cheng; Jong Kim; Anjan Debnath; Kirkwood M Land; Vipan Kumar
Journal:  Medchemcomm       Date:  2017-09-19       Impact factor: 3.597

  4 in total

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