Synthesis of isonicotinic acid N′-arylidene- N-[2-oxo-2-(4-aryl-piperazin-1-yl)-ethyl]-hydrazides as antituberculosis agents

Synthesis and in vitro antituberculosis activity of new series of isonicotinic acid N′-arylidene- N-[2-oxo-2-(4-aryl-piperazin-1-yl)-ethyl]-hydrazide derivatives 6– 9 has been described. A new series of antituberculosis agents 6– 9 was designed, synthesized and evaluated for antituberculosis activit...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2005-03, Vol.15 (6), p.1573-1576
Main Authors: Sinha, Neelima, Jain, Sanjay, Tilekar, Ajay, Upadhayaya, Ram Shankar, Kishore, Nawal, Jana, Gour Hari, Arora, Sudershan K.
Format: Article
Language:English
Subjects:
2-Oxo-2-(4-aryl-piperazin-1-yl)-ethyl-substituent
Antibacterial agents
Antibiotics. Antiinfectious agents. Antiparasitic agents
Antitubercular Agents - chemical synthesis
Antitubercular Agents - pharmacology
Antituberculosis activity
Biological and medical sciences
Isonicotinic acid hydrazide derivatives
Isonicotinic Acids - chemical synthesis
Isonicotinic Acids - pharmacology
Medical sciences
Miscellaneous
Molecular Structure
Mycobacterium tuberculosis - drug effects
Pharmacology. Drug treatments
Structure-Activity Relationship
Synthesis
Tuberculosis
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Summary:Synthesis and in vitro antituberculosis activity of new series of isonicotinic acid N′-arylidene- N-[2-oxo-2-(4-aryl-piperazin-1-yl)-ethyl]-hydrazide derivatives 6– 9 has been described. A new series of antituberculosis agents 6– 9 was designed, synthesized and evaluated for antituberculosis activity against Mycobacterium tuberculosis H 37Rv and clinical isolates in an agar dilution method. Compound 9h showed comparable in vitro activity (MIC) to isoniazid against M. tuberculosis H 37Rv and clinical isolates (sensitive strains) and superior activity against resistant strains of M. tuberculosis.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2005.01.073