Letters in Drug Design & Discovery

Author(s): Vaibhav Rajoriya, Varsha Kashaw* and Sushil K. Kashaw*

DOI: 10.2174/1570180814666170727143806

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Design, Synthesis, Characterization and Antitubercular Screening of some New 1,2,4-Triazoles Derived from Isonicotinic Acid Hydrazides

Page: [451 - 462] Pages: 12

  • * (Excluding Mailing and Handling)

Abstract

Background: A new series of substituted 1,2,4-triazoles derivative were synthesized and characterized by IR, 1HNMR, 13CNMR spectra, mass spectroscopy and elemental analysis.

Methods: The isonicotinic acid hydrazide (INH) was used as starting material. These synthesized compounds were screened for antitubercular activities by Luciferase Reporter Phase (LRP) assay against drug sensitive reference strain (H37RV) and on S, H, R & E resistant M. tuberculosis (MDR) clinical isolate. First line drug Rifampicin and Isoniazid were used as standard drugs.

Result: The study revealed that all the screened compounds showed good to moderate activity except compounds 5b & 5q.

Conclusion: The antitubercular activity indicated that the substitution of groups at third and fourth position of 1,2,4-triazole potentiate the activity as compare to isoniazid and rifampicin.

Keywords: 1, 2, 4-triazoles, isonicotinic acid hydrazides, antitubercular activity, luciferase reporter phase (LRP) assay, mass spectroscopy, rifampicin, isoniazid.

Graphical Abstract