About this item:

11 Views | 5 Downloads

Keywords:

  • Science & Technology
  • Life Sciences & Biomedicine
  • Physical Sciences
  • Chemistry, Medicinal
  • Chemistry, Organic
  • Pharmacology & Pharmacy
  • Chemistry
  • Methicillin-resistant Staphylococcus aureus
  • Bithionol
  • CD437
  • Retinoid
  • Gram-negative bacteria
  • ANTIBIOTICS
  • BROAD

Addition of ethylamines to the phenols of bithionol and synthetic retinoids does not elicit activity in gram-negative bacteria

Tools:

Journal Title:

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Volume:

Volume 30, Number 9

Publisher:

, Pages 127099-127099

Type of Work:

Article

Abstract:

Our labs have demonstrated the activity of bithionol and synthetic retinoids against methicillin-resistant Staphylococcus aureus (MRSA), as well as their membrane-acting mechanism of action. However, the compounds lack activity in gram-negative species. Herein, we apply a known strategy for converting gram-positive agents into broad-spectrum therapies: addition of an alkylamine. By appending an alkylamine to the phenols of these known membrane disruptors, we test whether this approach is applicable to our compounds. Ultimately, biological testing in four MRSA strains and three gram-negative species showed abolished or diminished activity in all our analogs compared to their parent compounds and no gram-negative activity. Thus, we find that alkylamines would not elicit broad-spectrum activity from bithionol or CD437 derivatives.
Export to EndNote