Literature DB >> 24863844

Synthesis and antifilarial activity of chalcone-thiazole derivatives against a human lymphatic filarial parasite, Brugia malayi.

Koneni V Sashidhara1, K Bhaskara Rao2, Vikas Kushwaha3, Ram K Modukuri2, Richa Verma3, P K Murthy4.   

Abstract

Here we report the synthesis of novel chalcone-thiazole compounds and their antifilarial activity. The antifilarial properties of these hybrids were assessed against microfilariae as well as adult worms of Brugia malayi. Among all the synthesized compounds, only two compounds, namely 4g and 4n were identified to be promising in vitro. These active compounds were tested in B. malayi-jird (Meriones unguiculatus) and B. malayi-Mastomys coucha models. Compound 4n showed 100% embryostatic effect and 49% macrofilaricidal in jirds and M. coucha models, respectively. This study provides a new structural clue for the development of novel antifilarial lead molecules.
Copyright © 2014 Elsevier Masson SAS. All rights reserved.

Entities:  

Keywords:  Albendazole; Brugia malayi; Diethylcarbamazine; Ivermectin; Macrofilariae; Microfilariae

Mesh:

Substances:

Year:  2014        PMID: 24863844     DOI: 10.1016/j.ejmech.2014.05.029

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


  3 in total

1.  Antifilarial activity of caffeic acid phenethyl ester on Brugia pahangi in vitro and in vivo.

Authors:  Nazeh M Al-Abd; Zurainee Mohamed Nor; Quazim O Junaid; Marzida Mansor; M S Hasan; Mustafa Kassim
Journal:  Pathog Glob Health       Date:  2017-10-25       Impact factor: 2.894

2.  In vitro, in silico and in vivo studies of ursolic acid as an anti-filarial agent.

Authors:  Komal Kalani; Vikas Kushwaha; Pooja Sharma; Richa Verma; Mukesh Srivastava; Feroz Khan; P K Murthy; Santosh Kumar Srivastava
Journal:  PLoS One       Date:  2014-11-06       Impact factor: 3.240

3.  Antifilarial activity of diterpenoids from Taxodium distichum.

Authors:  Vikas Kushwaha; Kirti Saxena; Richa Verma; Shiv K Verma; Deepali Katoch; Neeraj Kumar; Brij Lal; P Kalpana Murthy; Bikram Singh
Journal:  Parasit Vectors       Date:  2016-05-31       Impact factor: 3.876

  3 in total

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