1458632-01-3Relevant academic research and scientific papers
Efforts toward broadening the spectrum of arylomycin antibiotic activity
Liu, Jian,Smith, Peter A.,Steed, Danielle Barrios,Romesberg, Floyd
, p. 5654 - 5659 (2013/10/01)
New antibiotics are needed, and one source may be 'latent' antibiotics, natural products whose once broad-spectrum activity is currently limited by the evolution of resistance in nature. We have identified a potential class of latent antibiotics, the arylomycins, which are lipopeptides with a C-terminal macrocycle that target signal peptidase and whose spectrum is limited by a resistance-conferring mutation in many bacteria. Herein, we report the synthesis and evaluation of several arylomycin derivatives, and demonstrate that both C-terminal homologation with a glycyl aldehyde and addition of a positive charge to the macrocycle increase the activity and spectrum of the arylomycin scaffold.
