Approximately one-fourth of the world’s population is infected by Mycobacterium tuberculosis according to the WHO 2019 Global Tuberculosis Report. Of those infected, an average of 90% remain in the latent (inactive) form of the infection. Despite only 10% of those infected experiencing the active form of the infection, Tuberculosis (TB) is the top cause of death by infectious disease worldwide. Along with the great difficulty of treating the latent form of the disease and the lack of defined mechanisms for activation of TB from its dormant state, anti-microbial resistance (AMR) has amplified the severity of the TB epidemic. Of the first-line treatments for TB, rifampicin is the most effective. In 2018, there were approximately half a million new cases of rifampicin-resistant TB. Of these cases, 78% were multidrug-resistant TB, and of those 6.2% were extensively drug resistant. With a treatment success rate of only about 56%, the worldwide epidemic of TB is demanding a response. There is a great need for preventative treatment and new antibiotics to keep up with the rapid progression of AMR. Studies have shown the anti-tubercular potential of 1,2,3 triazole-based inhibitors, of synthetic and natural product-based tricyclic agents, as well as of the two moieties combined in a molecular hybridization approach. Fluorine has many unique properties including its high electronegativity, small size, and Van der Waals radius comparable to that of hydrogen. With these properties, fluorine has shown that when used as a bioisostere in different drug analogs, it can increase metabolic stability, bioavailability, binding ability, and potency. Molecularly hybridized molecules have been selected and will be synthesized with a bioisosteric replacement of the 1,2,3-triazole with the 5-fluoro-1,2,3-triazole. Each analog’s ability to inhibit the growth of Mycobacterium tuberculosis will be measured using a zone of inhibition test. By using the methods outlined above, we hope to see improved efficacy of these analogs as potential anti-tubercular agents.

Fluorinated triazoles as bioisosteres of amides and triazoles to improve efficacy of anti-tubercular analogs

Macromolecular Chemistry: The Second Century

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ACS Spring 2020 National Meeting & Expo

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.