Abstract
Objective: Novel aroylhydrazone schiff bases were synthesized and were screened for their biological activities.Methods: Using HCl as a catalyst, all the compounds were synthesized at room temperature and were characterized by IR and NMR techniques. The synthesized Schiff bases were screened for antibacterial, antifungal activities. In silico molecular docking, method was performed to study their anti-tuberculosis activity against enoyl acyl carrier protein reductase (InhA) from Mycobacterium tuberculosis (PDB id: 2NSD). Results: Compound P1 showed good antibacterial activity against gram positive (S. aureus) and gram negative (E. coli) bacterial strains and compound J1 showed good antifungal activity against A. niger. Molecular docking results reveal that compound B1 made two numbers of electrostatic interactions with 2NSD with more negative C docker interaction value. This indicated that the compound B1 was more active with minimum binding potential which is comparable with that of standard compound isoniazid.Conclusion: Aroylhydrazones having good biologically activities compared to that of standards were prepared.
Highlights
Tuberculosis (TB) “19th-century illness” could be a high communicable killer disease
Keeping the various biological applications of hydrazones in mind and in continuation of our earlier research [13], in the present study we reported novel biologically active hydrazone shiff bases using 2,4,5-trifluorobenzaldehyde as a source of the carbonyl compound
Aroylhydrazide derivatives were synthesized via condensation reaction by Schiff base route
Summary
Tuberculosis (TB) “19th-century illness” could be a high communicable killer disease. In 2014, 9.6 million individuals fell sick with TB and 1.5 million died from the malady. Over ninety-fifth of TB deaths occur in low and middle-income countries, and it's among the highest five causes of death for women aged fifteen to forty-four. TB could be a leading killer of HIV-positive people: in 2015, one in three HIV deaths was because of TB. In 2014, associate calculable 480000 individuals developed multidrug-resistant TB (MDR-TB). TB epidemic by 2030 is among the health targets of the recently adopted sustainable development goals [1]
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