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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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  <dc:creator>Maisuria Harshkumar Rakeshbhai, Dr.Alok Pal Jain, Mr Rohit Soni</dc:creator>
  <dc:date>2022-07-05</dc:date>
  <dc:description>Objective: The objective of the paper was to synthesize and characterize new derivatives of thiazole-based pyrazole derivatives and evaluate them for the antitubercular activity.

Material and methods: 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, 1HNMR, 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. 

Result and Discussion: 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 δ 8.53, due to the chromen-2-one-4H proton. The characteristic peak of -NH proton was attributed at δ 12.02-12.03.  The MABA method depicted the efficacy of compound by MIC value in µg/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 µg/ml). Luciferase reporter phase assay result data suggested that at 100µg/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 3rd position of pyrazole with 4-chlorophenyl, 4-nitrophenyl and 4-methylphenyl substitution at 1st position of pyrazole have enhance the anti-tubercular potential.

Keywords: Anti-tubercular activity, LRP assay, MABA method, pyrazole, Thiazole </dc:description>
  <dc:identifier>https://zenodo.org/record/6798419</dc:identifier>
  <dc:identifier>10.5281/zenodo.6798419</dc:identifier>
  <dc:identifier>oai:zenodo.org:6798419</dc:identifier>
  <dc:relation>doi:10.5281/zenodo.6798418</dc:relation>
  <dc:rights>info:eu-repo/semantics/openAccess</dc:rights>
  <dc:rights>https://creativecommons.org/licenses/by/4.0/legalcode</dc:rights>
  <dc:title>SYNTHESIS AND CHARACTERIZATION OF NEW DERIVATIVES OF PYRAZOLE AND SCREENED FOR THEIR ANTITUBERCULAR POTENTIAL</dc:title>
  <dc:type>info:eu-repo/semantics/article</dc:type>
  <dc:type>publication-article</dc:type>
</oai_dc:dc>
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