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.
Letters in Drug Design & Discovery
Title:Design, Synthesis, Characterization and Antitubercular Screening of some New 1,2,4-Triazoles Derived from Isonicotinic Acid Hydrazides
Volume: 15 Issue: 5
Author(s): Vaibhav Rajoriya, Varsha Kashaw*Sushil K. Kashaw*
Affiliation:
- SVN Institute of Pharmaceutical Sciences, SVN University, Sagar, M.P,India
- Department of Pharmaceutical Sciences, Dr. Harisingh Gour University (A Central University), Sagar, M.P,India
Keywords: 1, 2, 4-triazoles, isonicotinic acid hydrazides, antitubercular activity, luciferase reporter phase (LRP) assay, mass spectroscopy, rifampicin, isoniazid.
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.
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Cite this article as:
Rajoriya Vaibhav , Kashaw Varsha *, Kashaw K. Sushil *, Design, Synthesis, Characterization and Antitubercular Screening of some New 1,2,4-Triazoles Derived from Isonicotinic Acid Hydrazides, Letters in Drug Design & Discovery 2018; 15 (5) . https://dx.doi.org/10.2174/1570180814666170727143806
DOI https://dx.doi.org/10.2174/1570180814666170727143806 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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