Synthesis of 3,5-Bis(trifluoromethyl)phenyl-Substituted Pyrazole Derivatives as Potent Growth Inhibitors of Drug-Resistant Bacteria

oleh: Ibrahim S. Alkhaibari, Hansa Raj KC, Subrata Roy, Mohd. K. Abu-gazleh, David F. Gilmore, Mohammad A. Alam

Format: Article
Diterbitkan: MDPI AG 2021-08-01

Deskripsi

Enterococci and methicillin-resistant <i>S. aureus</i> (MRSA) are among the menacing bacterial pathogens. Novel antibiotics are urgently needed to tackle these antibiotic-resistant bacterial infections. This article reports the design, synthesis, and antimicrobial studies of 30 novel pyrazole derivatives. Most of the synthesized compounds are potent growth inhibitors of planktonic Gram-positive bacteria with minimum inhibitory concertation (MIC) values as low as 0.25 µg/mL. Further studies led to the discovery of several lead compounds, which are bactericidal and potent against MRSA persisters. Compounds <b>11</b>, <b>28</b>, and <b>29</b> are potent against <i>S. aureus</i> biofilms with minimum biofilm eradication concentration (MBEC) values as low as 1 µg/mL.