Marinopyrrole derivatives as potential antibiotic agents against methicillin-resistant staphylococcus aureus (II)

Chunwei Cheng, Yan Liu, Hao Song, Lili Pan, Jerry Li, Yong Qin, Rongshi Li

Research output: Contribution to journalArticle

17 Scopus citations

Abstract

Methicillin-resistant Staphylococcus aureus (MRSA) continues to be a major problem, causing severe and intractable infections worldwide. MRSA is resistant to all beta-lactam antibiotics, and alternative treatments are limited. A very limited number of new antibiotics have been discovered over the last half-century, novel agents for the treatment of MRSA infections are urgently needed. Marinopyrrole A was reported to show antibiotic activity against MRSA in 2008. After we reported the first total synthesis of (±)-marinopyrrole A, we designed and synthesized a series of marinopyrrole derivatives. Our structure activity relationship (SAR) studies of these novel derivatives against a panel of Gram-positive pathogens in antibacterial assays have revealed that a para-trifluoromethyl analog (33) of marinopyrrole A is ≥63-, 8-, and 4-fold more potent than vancomycin against methicillin-resistant Staphylococcus epidermidis (MRSE), methicillin-susceptible Staphylococcus aureus (MSSA) and MRSA, respectively. The results provide valuable information in the search for new-generation antibiotics.

Original languageEnglish (US)
Pages (from-to)2927-2948
Number of pages22
JournalMarine Drugs
Volume11
Issue number8
DOIs
Publication statusPublished - Aug 1 2013

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Keywords

  • Antibiotics
  • MRSA
  • MRSE
  • MSSA
  • Marinopyrroles
  • SAR

ASJC Scopus subject areas

  • Drug Discovery

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