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

Abstract

Heterosiklik hidrazon yapısı antitüberküloz aktiviteleri nedeniyle medisinal kimyacıların dikkatini çeken, cazip biyolojik olarak aktif önemli bir ilaç sınıfıdır. Bu amaçla, yeni hidrazon türevleri sentezlendi ve antitüberküloz etkinlikleri değerlendirilmiştir. (5,6,7,8-Tetrahidronaftalen-1-il) asetik asit hidraziti ile çeşitli benzaldehitlerin reaksiyonu, 5,6,7,8-tetrahidronaftalen asetik asit benziliden hidrazit türevlerini verdi. Bileşiklerin kimyasal yapıları 1H-NMR, EI-MS spectral verileri ve elemental analiz metodları ile aydınlatıldı. BACTEC 460 radyometrik sistem ve BACTEC 12B ortamından yararlanılarak Mycobacterium tuberculosis H37Rv (ATCC 27294)’e karşı bileşiklerin antitüberküloz aktiviteleri değerlendirilmiştir. Bileşik A10 yüksek antitüberküloz etkinlik (IC50: 3.072 μg/mL ve IC90: 3.358 μg/mL) ve düşük sitotoksisite (CC50: >40 μg/mL) gösterdi

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

Abstract

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

Keywords

• Hydrazone, Antituberculosis activity, Mycobacterium tuberculosis

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