Literature DB >> 25147153

1H-1,2,3-triazole tethered mono- and bis-ferrocenylchalcone-β-lactam conjugates: synthesis and antimalarial evaluation.

Kewal Kumar1, Bruno Pradines2, Marilyn Madamet3, Rémy Amalvict3, Vipan Kumar4.   

Abstract

A series of ferrocenylchalcone-β-lactam conjugates were synthesized and evaluated against 3D7 (CQ-Sensitive) and W2 (CQ-Resistant) strains of Plasmodium falciparum. The SAR studies revealed the dependence of activities at N-1 substituent of β-lactam ring with compounds being more potent on resistant strain. The compound 9f and 9l with N-cyclohexyl substituent proved to be the most potent and non-cytotoxic among the series exhibiting IC50 values of 2.36 and 2.43 μM respectively, against W2 strain of P. falciparum.
Copyright © 2014 Elsevier Masson SAS. All rights reserved.

Entities:  

Keywords:  1H-1,2,3-triazoles; Click chemistry; Ferrcenylchalcone-β-lactam conjugates; Plasmodium falciparum; Structure–activity relationship

Mesh：

Substances：

Year:  2014        PMID： 25147153     DOI： 10.1016/j.ejmech.2014.08.053

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


  7 in total

1.  Synthesis and antimicrobial evaluation of ester-linked 1,4-disubstituted 1,2,3-triazoles with a furyl/thienyl moiety.

Authors:  C P Kaushik; Raj Luxmi; Dharmendra Singh; Ashwani Kumar
Journal:  Mol Divers       Date:  2016-11-29       Impact factor: 2.943

Review 2.  An epigrammatic status of the 'azole'-based antimalarial drugs.

Authors:  Mousmee Sharma; Parteek Prasher
Journal:  RSC Med Chem       Date:  2019-12-23

3.  Insights into the interaction of potent antimicrobial chalcone triazole analogs with human serum albumin: spectroscopy and molecular docking approaches.

Authors:  Priyanka Yadav; Jitendra Kumar Yadav; Alka Agarwal; Satish K Awasthi
Journal:  RSC Adv       Date:  2019-10-08       Impact factor: 4.036

4.  Metal-chloroquine derivatives as possible anti-malarial drugs: evaluation of anti-malarial activity and mode of action.

Authors:  Maribel Navarro; William Castro; Marilyn Madamet; Rémy Amalvict; Nicolas Benoit; Bruno Pradines
Journal:  Malar J       Date:  2014-12-03       Impact factor: 2.979

5.  Malaria, tuberculosis and HIV: what's new? Contribution of the Institut Hospitalo-Universitaire Méditerranée Infection in updated data.

Authors:  Lionel Almeras; Leonardo K Basco; Cheikh Sokhna; Stéphane Ranque; Philippe Parola; Christian Devaux; Philippe Brouqui; Michel Drancourt; Bruno Pradines
Journal:  New Microbes New Infect       Date:  2018-07-04

6.  1H-1,2,3-triazole tethered isatin-ferrocene conjugates: Synthesis and in vitro antimalarial evaluation.

Authors:  Kewal Kumar; Bruno Pradines; Marilyn Madamet; Rémy Amalvict; Nicolas Benoit; Vipan Kumar
Journal:  Eur J Med Chem       Date:  2014-10-13       Impact factor: 6.514

Review 7.  Combination Therapy Strategies for the Treatment of Malaria.

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

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