Volume : 09, Issue : 07, July – 2022
Title:
03.SYNTHESIS AND CHARACTERIZATION OF NEW DERIVATIVES OF PYRAZOLE AND SCREENED FOR THEIR ANTITUBERCULAR POTENTIAL
Authors :
Maisuria Harshkumar Rakeshbhai, Dr.Alok Pal Jain, Mr Rohit Soni
Abstract :
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
Cite This Article:
Please cite this article in press Maisuria Harshkumar Rakeshbhai et al, Synthesis And Characterization Of New Derivatives Of Pyrazole And Screened For Their Antitubercular Potential, Indo Am. J. P. Sci, 2022; 09(7).,
Number of Downloads : 10
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