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

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

Bioorganic & medicinal chemistry letters (2010-07-10)
Dharmarajan Sriram, Perumal Yogeeswari, Devambatla Ravi Kumar Vyas, Palaniappan Senthilkumar, Pritesh Bhat, Madala Srividya
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.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
Rifampicin, suitable for plant cell culture, BioReagent, ≥95% (HPLC), powder or crystals
Sigma-Aldrich
5-Nitro-2-furoic acid, 98%
Sigma-Aldrich
Rifampicin, ≥95% (HPLC), powder or crystals
Supelco
Isoniazid, analytical standard, ≥99% (TLC)