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

IR@CDRI: CSIR-Central Drug Research Institute, Lucknow

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Field Value
 
Creator Sashidhara, K V
Rao, K B
Kushwaha, Vikas
Modukuri, R K
Verma, Richa
Murthy, P K
 
Date 2014-08-29T06:11:44Z
2014-08-29T06:11:44Z
2014
 
Identifier European Journal of Medicinal Chemistry, 2014, 81, 473-80
http://hdl.handle.net/123456789/1385
 
Description 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.
 
Format 378141 bytes
application/pdf
 
Language en
 
Relation CSIR-CDRI Communication No.8684
 
Subject Brugia malayi
Microfilariae
Macrofilariae
Diethylcarbamazine
Albendazole
Ivermectin
 
Title Synthesis and antifilarial activity of chalcone-thiazole derivatives against a human lymphatic filarial parasite, Brugia malayi
 
Type Article