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Microwave-Assisted Preparation of 1-Aryl-1H-pyrazole-5-amines
Published on: June 23, 2019
Síntesis, Acoplamiento y Estudios Biológicos de Derivados de Pirazina como Agentes Antimicobacterianos
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).
