Synthesis of some novel hydrazone derivatives and evaluation of their antituberculosis activity

被引:7
|
作者
Ozdemir, Ahmet [1 ]
Kaplancikli, Zafer Asim [1 ]
Turan-Zitouni, Gulhan [1 ]
Revial, Gilbert [2 ]
机构
[1] Anadolu Univ, Eczacil Fak, Farmasot Kimya, Eskisehir, Turkey
[2] UMR CNRS 7084, Cnam, Lab Transformat Chim & Pharmaceut, F-75003 Paris, France
关键词
Hydrazone; Antituberculosis activity; Mycobacterium tuberculosis;
D O I
10.12991/201014453
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The heterocyclic hydrazone constitute an important class of biologically active drug molecules which have attractive attention of medicinal chemists due to their antituberculosis activities. For this purpose, new hydrazone derivatives were synthesized and evaluated for antituberculosis activity. The reaction of (5,6,7,8-tetrahydronaphthalen-1-yl) acetic acid hydrazide with various benzaldehydes gave 5,6,7,8-tetrahydronaphtalen acetic acid benzylidene hydrazide derivatives. The chemical structures of the compounds were elucidated by 1H-NMR, EI-MS spectral data and Elemental Analysis. The compounds were evaluated for antituberculosis activity against Mycobacterium tuberculosis H37Rv (ATCC 27294) using the BACTEC 460 radiometric system and BACTEC 12B medium. The preliminary results indicated that all of the tested compounds showed low activity against the test organism. The compound A10 showed high antituberculosis activity (IC50: 3.072 mu g/mL and IC90: 3.358 g/mL) and low cytotoxicity (CC50: > 40 mu g/mL).
引用
收藏
页码:79 / 83
页数:5
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