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Synthesis, characterization and evaluation of new thiazole derivatives as anthelmintic agents

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Title Synthesis, characterization and evaluation of new thiazole derivatives as anthelmintic agents
 
Creator Guduru, Sai Krishna
Kumaraswamy, D
Sirisha, K
Santhoshi, K Sai
 
Subject Anthelmintic activity
Pheretima postuma
Molecular docking
Thiazole derivatives
β-tubulin protein
 
Description 616-623
A series of 2-amino substituted 4-phenyl thiazole derivatives has been synthesized by the conventional method. The thiazole derivatives have been synthesized by three steps. The obtained five derivatives have been purified by recrystallization process by using methanol as solvent and column chromatography [IVd Compound] and have been characterized by melting point, TLC, FTIR, 1H NMR and mass spectral data. All the five derivatives have been evaluated using in silico studies by using different softwares (Lipinski’s Rule of 5, OSIRIS molecular property explorer, Molsoft molecular property explorer, PASS and docking studies). These compounds have then been evaluated for anthelmintic activity against Indian adult earth worms (Pheretima postuma). All the compounds show significant anthelmintic activity. The compound IVc and IVe are shown to be potent compounds when compared with the standard drug (Mebendazole). Molecular docking studies have guided and prove the biological activity of the sythesised compounds against beta tubulin protein (1OJ0).
 
Date 2021-04-15T04:52:21Z
2021-04-15T04:52:21Z
2021-04
 
Type Article
 
Identifier 0975-0983(Online); 0376-4699(Print)
http://nopr.niscair.res.in/handle/123456789/57101
 
Language en_US
 
Rights CC Attribution-Noncommercial-No Derivative Works 2.5 India
 
Publisher NISCAIR-CSIR, India
 
Source IJC-B Vol.60B(04) [April 2021]