5-Nitro-2-furoic acid hydrazones: Design,synthesis and in vitro antimycobacterial evaluation against log and starved phase cultures |
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| Authors: | Dharmarajan Sriram Perumal Yogeeswari Devambatla Ravi Kumar Vyas Palaniappan Senthilkumar Pritesh Bhat Madala Srividya |
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| Institution: | Medicinal Chemistry & Antimycobacterial Research Laboratory, Pharmacy Group, Birla Institute of Technology & Science—Pilani, Hyderabad Campus, Jawahar Nagar, Hyderabad—500 078, Andhra Pradesh, India |
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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 μM against log- and starved-phase culture of MTB. Compound 4o also showed good enzyme inhibition of MTB ICL at 10 μM. The docking studies also confirmed the binding potential of the compounds at the ICL active site. |
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