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Details

Autor(en) / Beteiligte
Titel
Compound Uptake into E. coli Can Be Facilitated by N -Alkyl Guanidiniums and Pyridiniums
Ist Teil von
  • ACS infectious diseases, 2021-01, Vol.7 (1), p.162-173
Ort / Verlag
United States
Erscheinungsjahr
2021
Quelle
MEDLINE
Beschreibungen/Notizen
  • Multidrug-resistant Gram-negative bacterial infections are on the rise, and with no FDA approvals for new classes of broad-spectrum antibiotics in over 50 years, these infections constitute a major threat to human health. A significant challenge is the inability of most compounds to accumulate in Gram-negative bacteria. Recently developed predictive guidelines show that appending a primary amine to an appropriately shaped compound can enhance Gram-negative accumulation. Here, we report that other positively charged nitrogen functional groups, namely, -alkyl guanidiniums and pyridiniums, can also facilitate compound uptake into Gram-negative bacteria. The accumulation of a set of 60 nonantibiotic compounds, consisting of 20 primary amines and their corresponding guanidiniums and pyridiniums, was assessed in . We also installed these alternate functional groups onto antibiotic scaffolds and assessed their accumulation and antibacterial activity in Gram-negative bacteria. The results suggest that other positively-charged, nitrogen-containing functional groups should be considered when designing antibiotics with Gram-negative activity.
Sprache
Englisch
Identifikatoren
ISSN: 2373-8227
eISSN: 2373-8227
DOI: 10.1021/acsinfecdis.0c00715
Titel-ID: cdi_pubmedcentral_primary_oai_pubmedcentral_nih_gov_7796962

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