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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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    <subfield code="a">SYNTHESIS AND CHARACTERIZATION OF NEW DERIVATIVES OF PYRAZOLE AND SCREENED FOR THEIR ANTITUBERCULAR POTENTIAL</subfield>
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    <subfield code="a">&lt;p&gt;&lt;strong&gt;&lt;em&gt;Objective:&lt;/em&gt;&lt;/strong&gt;&lt;em&gt; The objective of the paper was to synthesize and characterize new &lt;em&gt;derivatives of thiazole-based pyrazole derivatives and evaluate them for the antitubercular activity.&lt;/em&gt;&lt;/em&gt;&lt;/p&gt;

&lt;p&gt;&lt;strong&gt;&lt;em&gt;Material and methods:&lt;/em&gt;&lt;/strong&gt;&lt;em&gt; 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, &lt;sup&gt;1&lt;/sup&gt;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. &lt;/em&gt;&lt;/p&gt;

&lt;p&gt;&lt;strong&gt;&lt;em&gt;Result and Discussion:&lt;/em&gt;&lt;/strong&gt;&lt;em&gt; 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 &amp;delta; 8.53, due to the chromen-2-one-4H proton. The characteristic peak of -NH proton was attributed at &amp;delta; 12.02-12.03. &amp;nbsp;The MABA method depicted the efficacy of compound by MIC value in &amp;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 &amp;micro;g/ml). Luciferase reporter phase assay result data suggested that at 100&amp;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&lt;sup&gt;rd&lt;/sup&gt; position of pyrazole with 4-chlorophenyl, 4-nitrophenyl and 4-methylphenyl substitution at 1&lt;sup&gt;st&lt;/sup&gt; position of pyrazole have enhance the anti-tubercular potential.&lt;/em&gt;&lt;/p&gt;

&lt;p&gt;&lt;strong&gt;Keywords: &lt;/strong&gt;&lt;em&gt;Anti-tubercular activity, LRP assay, MABA method, pyrazole, Thiazole &lt;/em&gt;&lt;/p&gt;</subfield>
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