PMID- 30185388
OWN - NLM
STAT- MEDLINE
DCOM- 20190507
LR  - 20190507
IS  - 1464-3391 (Electronic)
IS  - 0968-0896 (Linking)
VI  - 26
IP  - 17
DP  - 2018 Sep 15
TI  - Amphipathic sulfonamidobenzamides mimicking small antimicrobial marine natural 
      products; investigation of antibacterial and anti-biofilm activity against 
      antibiotic resistant clinical isolates.
PG  - 4930-4941
LID - S0968-0896(18)30897-6 [pii]
LID - 10.1016/j.bmc.2018.08.032 [doi]
AB  - There is an urgent need for novel antimicrobial agents to address the threat of 
      bacterial resistance to modern society. We have used a structural motif found in 
      antimicrobial marine hit compounds as a basis for synthesizing a library of 
      antimicrobial sulfonamidobenzamide lead compounds. Potent in vitro antimicrobial 
      activity against clinically relevant bacterial strains was demonstrated for two 
      compounds, G6 and J18, with minimal inhibitory concentrations (MIC) of 4-16 mug/ml 
      against clinical methicillin-resistant Staphylococcus aureus (MRSA) and 
      vancomycin-resistant Enterococcus faecium (VRE). The two compounds G6 and J18, 
      together with several other compounds of this library, also caused >/=90% 
      eradication of pre-established biofilm of methicillin-resistant S. epidermidis 
      (MRSE) at 40 mug/ml. Using a luciferase assay, the mechanism of action of G6 was 
      shown to resemble the biocide chlorhexidine by targeting the bacterial cell 
      membrane.
CI  - Copyright (c) 2018 Elsevier Ltd. All rights reserved.
FAU - Igumnova, Elizaveta M
AU  - Igumnova EM
AD  - Department of Pharmacy, Faculty of Health Sciences, UiT - The Arctic University 
      of Norway, NO-9037 Tromso, Norway.
FAU - Mishchenko, Ekaterina
AU  - Mishchenko E
AD  - The Norwegian College of Fishery Science, Faculty of Biosciences, Fisheries and 
      Economics, UiT - The Arctic University of Norway, NO-9037 Tromso, Norway.
FAU - Haug, Tor
AU  - Haug T
AD  - The Norwegian College of Fishery Science, Faculty of Biosciences, Fisheries and 
      Economics, UiT - The Arctic University of Norway, NO-9037 Tromso, Norway.
FAU - Blencke, Hans-Matti
AU  - Blencke HM
AD  - The Norwegian College of Fishery Science, Faculty of Biosciences, Fisheries and 
      Economics, UiT - The Arctic University of Norway, NO-9037 Tromso, Norway.
FAU - Sollid, Johanna U Ericson
AU  - Sollid JUE
AD  - Department of Medical Biology, Faculty of Health Sciences, UiT - The Arctic 
      University of Norway, NO-9037 Tromso, Norway.
FAU - Fredheim, Elizabeth G Aarag
AU  - Fredheim EGA
AD  - Department of Pharmacy, Faculty of Health Sciences, UiT - The Arctic University 
      of Norway, NO-9037 Tromso, Norway.
FAU - Lauksund, Silje
AU  - Lauksund S
AD  - Department of Pharmacy, Faculty of Health Sciences, UiT - The Arctic University 
      of Norway, NO-9037 Tromso, Norway.
FAU - Stensvag, Klara
AU  - Stensvag K
AD  - The Norwegian College of Fishery Science, Faculty of Biosciences, Fisheries and 
      Economics, UiT - The Arctic University of Norway, NO-9037 Tromso, Norway.
FAU - Strom, Morten B
AU  - Strom MB
AD  - Department of Pharmacy, Faculty of Health Sciences, UiT - The Arctic University 
      of Norway, NO-9037 Tromso, Norway. Electronic address: morten.strom@uit.no.
LA  - eng
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
DEP - 20180828
PL  - England
TA  - Bioorg Med Chem
JT  - Bioorganic & medicinal chemistry
JID - 9413298
RN  - 0 (Anti-Bacterial Agents)
RN  - 0 (Benzamides)
RN  - 0 (Biological Products)
RN  - 0 (Sulfonamides)
SB  - IM
MH  - Anti-Bacterial Agents/chemistry/*pharmacology
MH  - Benzamides/chemistry/*pharmacology
MH  - Biofilms/*drug effects
MH  - Biological Products/chemistry/*pharmacology
MH  - Drug Resistance, Multiple, Bacterial
MH  - Erythrocytes/drug effects
MH  - Gram-Negative Bacteria/*drug effects
MH  - Gram-Positive Bacteria/*drug effects
MH  - Hemolysis/drug effects
MH  - Humans
MH  - Methicillin-Resistant Staphylococcus aureus/*drug effects
MH  - Microbial Sensitivity Tests
MH  - Seawater/chemistry
MH  - Sulfonamides/chemistry/*pharmacology
OTO - NOTNLM
OT  - Antibacterial
OT  - Antimicrobial
OT  - ESBL - CARBA
OT  - Marine natural product mimics
OT  - Multi-resistant bacteria
OT  - Peptidomimetics
OT  - Sulfonamidobenzamides
EDAT- 2018/09/07 06:00
MHDA- 2019/05/08 06:00
CRDT- 2018/09/07 06:00
PHST- 2018/05/09 00:00 [received]
PHST- 2018/08/22 00:00 [revised]
PHST- 2018/08/26 00:00 [accepted]
PHST- 2018/09/07 06:00 [pubmed]
PHST- 2019/05/08 06:00 [medline]
PHST- 2018/09/07 06:00 [entrez]
AID - S0968-0896(18)30897-6 [pii]
AID - 10.1016/j.bmc.2018.08.032 [doi]
PST - ppublish
SO  - Bioorg Med Chem. 2018 Sep 15;26(17):4930-4941. doi: 10.1016/j.bmc.2018.08.032. 
      Epub 2018 Aug 28.