Synthesis of some novel hydrazone derivatives and evaluation of their antituberculosis activity [Bazi{dotless} yeni hidrazon türevlerinin sentezi ve bunlari{dotless}n antitüberküloz etkilerinin degerlendirilmesi]

Abstract

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 µg/mL and IC90: 3.358 µg/mL) and low cytotoxicity (CC50: >40 µg/mL).