RRC ID 55802
Author Durcik M, Lovison D, Skok Ž, Durante Cruz C, Tammela P, Tomašič T, Benedetto Tiz D, Draskovits G, Nyerges Á, Pál C, Ilaš J, Peterlin Mašič L, Kikelj D, Zidar N.
Title New N-phenylpyrrolamide DNA gyrase B inhibitors: Optimization of efficacy and antibacterial activity.
Journal Eur J Med Chem
Abstract value of 85 nM against E. coli DNA gyrase displays the most potent antibacterial activity, with MIC values of 1.56 μM against Enterococcus faecalis, and 3.13 μM against wild type S. aureus, methicillin-resistant S. aureus (MRSA) and vancomycin-resistant Enterococcus (VRE). The activity against wild type E. coli in the presence of efflux pump inhibitor phenylalanine-arginine β-naphthylamide (PAβN) is 4.6 μM.
Volume 154
Pages 117-132
Published 2018-6-25
DOI 10.1016/j.ejmech.2018.05.011
PII S0223-5234(18)30415-X
PMID 29778894
PMC PMC6016738
MeSH Amides / cerebrospinal fluid Amides / chemistry Amides / pharmacology* Anti-Bacterial Agents / chemical synthesis Anti-Bacterial Agents / chemistry Anti-Bacterial Agents / pharmacology* DNA Gyrase / metabolism* Dose-Response Relationship, Drug Enterococcus faecalis / drug effects* Escherichia coli / drug effects* Escherichia coli / enzymology Microbial Sensitivity Tests Molecular Structure Pyrroles / cerebrospinal fluid Pyrroles / chemistry Pyrroles / pharmacology* Staphylococcus aureus / drug effects* Staphylococcus aureus / enzymology Structure-Activity Relationship Topoisomerase II Inhibitors / chemical synthesis Topoisomerase II Inhibitors / chemistry Topoisomerase II Inhibitors / pharmacology*
IF 4.816
Prokaryotes E. coli JW5503, JD17464