Journal article Open Access

SYNTHESIS AND CHARACTERIZATION OF NEW DERIVATIVES OF PYRAZOLE AND SCREENED FOR THEIR ANTITUBERCULAR POTENTIAL

Maisuria Harshkumar Rakeshbhai, Dr.Alok Pal Jain, Mr Rohit Soni


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{
  "publisher": "Zenodo", 
  "DOI": "10.5281/zenodo.6798419", 
  "author": [
    {
      "family": "Maisuria Harshkumar Rakeshbhai, Dr.Alok Pal Jain, Mr Rohit Soni"
    }
  ], 
  "issued": {
    "date-parts": [
      [
        2022, 
        7, 
        5
      ]
    ]
  }, 
  "abstract": "<p><strong><em>Objective:</em></strong><em> The objective of the paper was to synthesize and characterize new <em>derivatives of thiazole-based pyrazole derivatives and evaluate them for the antitubercular activity.</em></em></p>\n\n<p><strong><em>Material and methods:</em></strong><em> The pyrazole derivatives have been synthesized by the two steps process in that first step pyrazole based carbothioamide compounds was synthesized and it further reacted with 3-(2-bromoacetyl)-2H-chromen-2-one to from the final compounds. Total Fourteen compounds have been synthesized and characterized by IR, <sup>1</sup>HNMR, elemental analysis and mass spectral analysis. The final Compounds (TP-1 to TP-14) have been evaluated for antitubercular activity by two Ex-vivo method i.e. LRP assay and MABA method. </em></p>\n\n<p><strong><em>Result and Discussion:</em></strong><em> IR analysis of compound TP-1 to TP-14 showed the occurrence of the characteristics peak at 3415-3420 (-NH), 1717-1721 (-C=O) and 1627 (-C=N). The 1H-NMR spectrum shown a singlet peak at &delta; 8.53, due to the chromen-2-one-4H proton. The characteristic peak of -NH proton was attributed at &delta; 12.02-12.03. &nbsp;The MABA method depicted the efficacy of compound by MIC value in &micro;g/ml; five compounds i.e. TP-8 (1.75), TP-3 (1.75), TP-9 (2.50), TP-10 (2.25), and TP-1 (2.25) have shown lowest MIC among all other compounds and it was similarly active with the standard anti-TB drug Isoniazid (MIC value 1.25 &micro;g/ml). Luciferase reporter phase assay result data suggested that at 100&micro;g/ml concentration, 10 compounds (TP-1, TP-2, TP-3, TP-4, TP-5, TP-8, TP-9, TP-10 TP-11 and TP-12) shown the potent anti-tubercular activity. Structure activity relationship (SAR) of the compound indicated that 4-chlorophenyl substitution at 3<sup>rd</sup> position of pyrazole with 4-chlorophenyl, 4-nitrophenyl and 4-methylphenyl substitution at 1<sup>st</sup> position of pyrazole have enhance the anti-tubercular potential.</em></p>\n\n<p><strong>Keywords: </strong><em>Anti-tubercular activity, LRP assay, MABA method, pyrazole, Thiazole </em></p>", 
  "title": "SYNTHESIS AND CHARACTERIZATION OF NEW DERIVATIVES OF PYRAZOLE AND SCREENED FOR THEIR ANTITUBERCULAR POTENTIAL", 
  "type": "article-journal", 
  "id": "6798419"
}
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