Abstract
The in vitro activities of five quinazolinone antibacterials, compounds Q1 to Q5, were tested against 210 strains of methicillin-resistant Staphylococcus aureus (MRSA). The MIC50/MIC90 values (in μg/ml) were as follows: Q1, 0.5/2; Q2, 1/4; Q3, 2/4; Q4, 0.06/0.25; and Q5, 0.125/0.5. Several strains with high MIC values (from 8 to >32 μg/ml) for some of these compounds exhibited amino acid changes in the penicillin-binding proteins, which are targeted by these antibacterials.
Keywords:
MRSA; methicillin-resistant Staphylococcus aureus; penicillin-binding proteins; quinazolinones; staphylococci.
Copyright © 2019 Ceballos et al.
Publication types
-
Research Support, N.I.H., Extramural
-
Research Support, Non-U.S. Gov't
MeSH terms
-
Amino Acid Substitution
-
Anti-Bacterial Agents / chemistry
-
Anti-Bacterial Agents / pharmacology*
-
Humans
-
Methicillin-Resistant Staphylococcus aureus / drug effects*
-
Methicillin-Resistant Staphylococcus aureus / growth & development
-
Methicillin-Resistant Staphylococcus aureus / metabolism
-
Microbial Sensitivity Tests
-
Penicillin-Binding Proteins / genetics
-
Penicillin-Binding Proteins / metabolism
-
Quinazolinones / chemistry
-
Quinazolinones / pharmacology*
-
Spain
-
Staphylococcal Infections / drug therapy
-
Staphylococcal Infections / microbiology
Substances
-
Anti-Bacterial Agents
-
Penicillin-Binding Proteins
-
Quinazolinones