Synthesis and antibacterial activity of propylamycin derivatives

Propylamycin is a next-generation aminoglycoside antibiotic that displays increased antibacterial potency. But due to the hydroxy group in propylamycin 5′′-position, it is inactivated by aminoglycoside modifying enzymes. To overcome this problem groups led by prof. Edgars Suna (Latvian Institute of Organic Synthesis), Dr. Sven N. Hobbie (University of Zurich) and David Crich (University of Georgia)  have obtained various propylamycin derivatives functionalized at the 5′′- and other positions and analyzed their antibacterial activity.

Scientists found out that one derivative – 5′′-deoxy-5′′-formamidopropylamycin – displays excellent antibacterial activity and overcomes problems associated with aminoglycoside modifying enzymes.

This research is published in the journal ACS Infectious Diseases (IF=4.61).

Read the article:

Lubriks, D.; Zogota, R.; Sarpe, V.A.; Matsushita, T.; Sati, G.C.; Haldimann, K.; Gysin, M.; Böttger,E.C.; Vasella, A.; Suna,E.*; Hobbie, S.N.*; Crich, D.*
Synthesis and Antibacterial Activity of Propylamycin Derivatives Functionalized at the 5′′- and Other Positions with a View to Overcoming Resistance Due to Aminoglycoside Modifying Enzymes.
ACS Infect. Dis. , 2021. DOI: 10.1021/acsinfecdis.1c00158