Literature DB >> 25817773

Synthesis and in vitro antiplasmodial evaluation of 7-chloroquinoline-chalcone and 7-chloroquinoline-ferrocenylchalcone conjugates.

Raghu Raj1, Anu Saini1, Jiri Gut2, Philip J Rosenthal2, Vipan Kumar3.   

Abstract

The manuscript describes the synthesis of novel amide tethered 7-chloroquinoline-chalcone and 7-chloroquinoline-ferrocenylchalcone bifunctional hybrids and their evaluation as antimalarial agents against W2 resistant strain of Plasmodium falciparum. The antiplasmodial activity of 7-chloroquinoline-ferrocenylchalcones was found to be less than their corresponding simple chalcone conjugates. The presence of a methoxy substituent at para position of ring B on chalcones and longer alkyl chain length markedly improved the antiplasmodial profiles of the synthesized scaffolds with the most potent of the test compound exhibiting an IC50 value of 17.8 nM.
Copyright © 2015 Elsevier Masson SAS. All rights reserved.

Entities:  

Keywords:  7-Chloroquinoline; Antiplasmodial activity; Chalcone; Ferrocenylchalcone; IC(50) value

Mesh:

Substances:

Year:  2015        PMID: 25817773     DOI: 10.1016/j.ejmech.2015.03.045

Source DB:  PubMed          Journal:  Eur J Med Chem        ISSN: 0223-5234            Impact factor:   6.514


  3 in total

1.  Synthesis, Structure-Activity Relationship, and Antimalarial Efficacy of 6-Chloro-2-arylvinylquinolines.

Authors:  Guang Huang; Claribel Murillo Solano; Joel Melendez; Justin Shaw; Jennifer Collins; Robert Banks; Arash Keshavarzi Arshadi; Rachasak Boonhok; Hui Min; Jun Miao; Debopam Chakrabarti; Yu Yuan
Journal:  J Med Chem       Date:  2020-10-06       Impact factor: 7.446

Review 2.  Combination Therapy Strategies for the Treatment of Malaria.

Authors:  Sibusiso Alven; Blessing Aderibigbe
Journal:  Molecules       Date:  2019-10-07       Impact factor: 4.411

3.  Synthesis and Evaluation of Antiplasmodial Activity of 2,2,2-Trifluoroethoxychalcones and 2-Fluoroethoxy Chalcones against Plasmodium falciparum in Culture.

Authors:  Kavita Devi; Vinoth Rajendran; T M Rangarajan; Rishi Pal Singh; Prahlad C Ghosh; Manjula Singh
Journal:  Molecules       Date:  2018-05-14       Impact factor: 4.411

  3 in total

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