Research Paper on Derivatives of 3-(5-Nitrofuran-2-yl)prop-2-en-1-one with potent antituberculosis activity inhibit a novel therapeutic target in mycobacteria called arylamine N-acetyltransferase.

Description

Title: Derivatives of 3-(5-Nitrofuran-2-yl)prop-2-en-1-one with potent antituberculosis activity inhibit a novel therapeutic target in mycobacteria called arylamine N-acetyltransferase. 

Abstract: In order to determine their therapeutic index, the inhibitory potential of 3-(5-nitrofuran-2-yl)prop-2-en-1-one derivatives was assessed against a panel of bacteria as well as mammalian cell lines. In order to pinpoint their therapeutic target, we also looked into the derivatives’ antibiotic action mechanism. We found compound 2 to be a highly effective inhibitor of Mycobacterium tuberculosis H37Rv growth in vitro (MIC: 0.031 mg/L), outperforming the first-line antituberculosis medications currently in use, such as isoniazid, rifampicin, ethambutol, and pretomanid. Additionally, compound 3 was equally effective as pretomanid against a clinical isolate of M. tuberculosis that was multidrug resistant. The derivatives had a selective bactericidal effect on mycobacteria that grew slowly. With high selectivity indices, they displayed low cytotoxicity toward the murine RAW 264.7 and human THP-1 cell lines. In a macrophage model with intracellular mycobacterial infection, compound 1 successfully eliminated the mycobacteria. The derivatives were tested for their ability to inhibit mycobacterial arylamine N-acetyltransferase (NAT), a novel target crucial for M. tuberculosis’s intracellular survival, and they were found to be effective inhibitors of recombinant mycobacterial NAT. This research gave researchers new ideas for creating potent and targeted antituberculosis drugs with mycobacterial NAT inhibition as one of their potential endogenous mechanisms of action.

Keywords: tuberculosis; antibiotic resistance; 5-nitrofuran; arylamine N-acetyltransferase

Paper Quality: SCOPUS / Web of Science Level Research Paper

Subject: Antibiotics

Writer Experience: 20+ Years

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