Synthesis and biological evaluation of 1-(5-(2-chloroquinolin-3-yl)-3-phenyl-1H-pyrazol-1-yl)ethanone derivatives as potential antimicrobial agents

A novel series of 2-Chloroquinoline nucleus clubbed with the pyrazole ring has been synthesized and screened for antibacterial and antifungal activity. The results obtained were promising against both bacterial and fungal strains.   Among the series, compound MB-N was found moderately active against Aspergillus fumigatus, Penicillium notatum and Bacillus subtilis having MIC 48, 46 and 44 μg/ml, respectively whereas compound MB-A was found active against P. notatum, B. subtilis and Escherichia coli having MIC 57, 54 and 43 μg/ml, respectively as compared to standard

Overview of the Development of DprE1 Inhibitors for Combating the Menace of Tuberculosis

Decaprenylphosphoryl-β-d-ribose 2′-epimerase (DprE1), a vital enzyme for cell wall synthesis, plays a crucial role in the formation of lipoarabinomannan and arabinogalactan. It was first reported as a druggable target on the basis of inhibitors discovered in high throughput screening of a drug library. Since then, inhibitors with different types of chemical scaffolds have been reported for their activity against this enzyme. Formation of a covalent or noncovalent bond by the interacting ligand with the enzyme causes loss of its catalytic activity which ultimately leads to the death of the mycobacterium. This Perspective describes various DprE1 inhibitors as anti-TB agents reported to date