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Synthesis of benzothiazolopyrazoloisonicotinohydrazide derivatives and their nitro regioisomers for antitubercular activity

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Title Synthesis of benzothiazolopyrazoloisonicotinohydrazide derivatives and their nitro regioisomers for antitubercular activity
 
Creator Hazra, Kuntal
Nandha, B
 
Subject Nitrobenzothiazoles
Antitubercular activity
Pyrazole
Regioisomers
 
Description 1388-1399
The history of incessant struggle and the current global burden associated with emerging infectious disease especially tuberculosis, guided us to define the scope of this research project, and to identify research gaps in synthesizing some heterocyclic compounds for anti-tubercular activity. In this research project, we have synthesized a series of novel heterocyclic (benzothiazoles) compounds viz N'-((1-(7-chloro-6-fluorobenzo[d]thiazol-2-yl)-3-phenyl-1H-pyrazol-4-yl) methylene)isonicotinohydrazide 12a-c their 5-nitro 15a-c and 4-nitro 18a-c derivatives, by a series of reactions of their respective synthons. The completion of reaction and the purity of the synthesized compounds have been established by chromatographic analysis. All the newly synthesized compounds satisfactorily show acceptable analysis for their anticipated structures, which have been confirmed based on physicochemical and spectral data. These newly synthesized compounds have been primarily evaluated for their in vitro anti-tubercular activity by Ziehl-Neelsen stain method. Compounds 15a, 15b, 15c, 18b and 18c have shown 100% inhibition at 25 mg/ mL and MIC values of around 45 nM against M. tuberculosis H37Rv (ATCC 27294). Cytotoxicity on THP-1 cell line shows that all the tested compounds are safe.
 
Date 2020-10-09T05:11:50Z
2020-10-09T05:11:50Z
2020-09
 
Type Article
 
Identifier 0975-0983(Online); 0376-4699(Print)
http://nopr.niscair.res.in/handle/123456789/55446
 
Language en_US
 
Rights CC Attribution-Noncommercial-No Derivative Works 2.5 India
 
Publisher NISCAIR-CSIR, India
 
Source IJC-B Vol.59B(09) [September 2020]