Synthesis and characterization of novel hydrazide-hydrazones and the study of their structure-antituberculosis activity
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BEDIA, Koçyiit-Kaymakçiolu, ELÇIN, Oruç, SEDA, Unsalan, KANDEMIRLI, Fatma, SHVETS, Nathaly, ROLLAS, Sevim, DIMOGLO, Anatholy. Synthesis and characterization of novel hydrazide-hydrazones and the study of their structure-antituberculosis activity. In: European Journal of Medicinal Chemistry, 2006, vol. 41, pp. 1253-1261. ISSN 0223-5234. DOI: https://doi.org/10.1016/j.ejmech.2006.06.009
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European Journal of Medicinal Chemistry
Volumul 41 / 2006 / ISSN 0223-5234 /ISSNe 1768-3254

Synthesis and characterization of novel hydrazide-hydrazones and the study of their structure-antituberculosis activity

DOI:https://doi.org/10.1016/j.ejmech.2006.06.009

Pag. 1253-1261

Bedia Koçyiit-Kaymakçiolu1, Elçin Oruç1, Seda Unsalan1, Kandemirli Fatma2, Shvets Nathaly3, Rollas Sevim1, Dimoglo Anatholy34
 
1 Marmara University,
2 Kocaeli University,
3 Gebze Institute of Technology,
4 Institute of Applied Physics, Academy of Sciences of Moldova
 
 
Disponibil în IBN: 4 iulie 2023


Rezumat

A series of hydrazide-hydrazones, based on a series of 4-substituted benzoic acid, were synthesized, and their structures were elucidated and screened for the antituberculosis activity against Mycobacterium tuberculosis H37Rv with the help of the BACTEC 460 radiometric system. Compound 3, 4-fluorobenzoic acid [((5-nitro)thiophen-2yl) methylene]hydrazide showed the highest inhibitory activity in this series. The search of pharmacophores was done by means of the Electronic-Topological Method (ETM). The model developed in this study is supposed to be applied to the design, preparation and screening of new compounds of similar structure in order to further test and optimize the model with the eventual goal of preparing new anti-tubercular agents.

Cuvinte-cheie
antituberculosis activity, Hydrazide-hydrazones, Structure-activity relationships