Bioorganic & Medicinal Chemistry Letters 2010-08-01

5-Nitro-2-furoic acid hydrazones: design, synthesis and in vitro antimycobacterial evaluation against log and starved phase cultures.

Dharmarajan Sriram, Perumal Yogeeswari, Devambatla Ravi Kumar Vyas, Palaniappan Senthilkumar, Pritesh Bhat, Madala Srividya

Index: Bioorg. Med. Chem. Lett. 20 , 4313-6, (2010)

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Abstract

Various 5-nitro-2-furoic acid hydrazones were synthesized and evaluated for in vitro activities against log and starved phase culture of two mycobacterial species and Mycobacterium tuberculosis (MTB) isocitrate lyase (ICL) enzyme inhibition studies. Among twenty one compounds, 5-nitro-N'-[(5-nitro-2-furyl)methylidene]-2-furohydrazide (4o) was found to be the most active compound in vitro with MICs of 2.65 and 10.64 microM against log- and starved-phase culture of MTB. Compound 4o also showed good enzyme inhibition of MTB ICL at 10 microM. The docking studies also confirmed the binding potential of the compounds at the ICL active site.Copyright 2010 Elsevier Ltd. All rights reserved.