Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10587623 | Bioorganic & Medicinal Chemistry Letters | 2013 | 6 Pages |
Abstract
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.
Keywords
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Jian Liu, Peter A. Smith, Danielle Barrios Steed, Floyd Romesberg,