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<p class="TitleMain">Synthesis of benzothiazolopyrazoloisonicotinohydrazide derivatives and their nitro regioisomers for antitubercular activity</p><br />

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Title Statement <p class="TitleMain">Synthesis of benzothiazolopyrazoloisonicotinohydrazide derivatives and their nitro regioisomers for antitubercular activity</p><br />
 
Added Entry - Uncontrolled Name Hazra, Kuntal ; AICTE, PCI, MAKAUT, West Bengal
Nandha, B ; Department of Pharmaceutical Chemistry, Vivekananda College of Pharmacy, Bangalore 560 055, India
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Uncontrolled Index Term Nitrobenzothiazoles, antitubercular activity, pyrazole, regioisomers
 
Summary, etc. <p class="Abstract">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 <em>viz</em> <em>N'</em>-((1-(7-chloro-6-fluorobenzo[<em>d</em>]thiazol-2-yl)-3-phenyl-1<em>H</em>-pyrazol-4-yl)<br /> methylene)isonicotinohydrazide <strong>12a-c</strong> their 5-nitro <strong>15a-c</strong> and 4-nitro <strong>18a-c</strong> 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 <em>in vitro</em> anti-tubercular activity by Ziehl-Neelsen stain method. Compounds <strong>15a</strong>, <strong>15b</strong>, <strong>15c</strong>, <strong>18b</strong> and <strong>18c</strong> have shown 100% inhibition at 25 mg/ mL and MIC values of around 45 nM against <em>M. tuberculosis</em> H<sub>37</sub>Rv (ATCC 27294). Cytotoxicity on THP-1 cell line shows that all the tested compounds are safe.</p><p> </p>
 
Publication, Distribution, Etc. Indian Journal of Chemistry -Section B (IJC-B)
2020-11-10 12:16:00
 
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http://op.niscair.res.in/index.php/IJCB/article/view/28942
 
Data Source Entry Indian Journal of Chemistry -Section B (IJC-B); ##issue.vol## 59, ##issue.no## 9 (2020): Indian Journal of Chemistry Section - B (IJCB)
 
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Nonspecific Relationship Entry http://op.niscair.res.in/index.php/IJCB/article/download/28942/465489096
http://op.niscair.res.in/index.php/IJCB/article/download/28942/0
 
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