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Microwave-Assisted Preparation of 1-Aryl-1H-pyrazole-5-amines
Published on: June 23, 2019
Synthesis, Docking, and Biological Studies of Pyrazine Derivatives as Antimycobacterial Agents
Nagaraja Reddy Gangarapu1,2, Archakam Ranganatham3, Eeda Koti Reddy4
1Department of Chemistry, Government Science College, 560001, Bengaluru, Karnataka, India.
Introduction:
A series of novel 2-((3,5-diphenylpyrazin-2-yl)amino)-1-(piperidin-1- yl/pyrrolidin-1-yl)ethanone derivatives (5a-5l) were synthesized and evaluated for their tuberculosis activity using the standard strain H37Rv and two other clinically isolated multidrug-resistant strains with different resistances.
Methods:
All compounds 5a-5l showed promising results in tuberculosis activity. Among them, 5g and 5i demonstrated remarkable activity at 5 μg/mL against H37Rv and three other MDR strains. The compounds 5c, 5d, and 5f were sensitive, showing inhibition between 15-25 μg/mL against M. tuberculosis growth. In-silico docking studies were conducted for 5a-5l using the 2FUM protein of M. tuberculosis.
Results:
These studies revealed that compounds 5g and 5i exhibited strong interactions with the MTB protein, with binding energies of -9.85 kcal/mol and -10.74 kcal/mol, respectively, and inhibitory concentrations of 0.38 μM and 0.77 μM.
Conclusion:
Moreover, these motifs also displayed good binding energy coupled with favorable minimum inhibitory concentrations (MIC).
