SwePub
Sök i LIBRIS databas

  Extended search

WFRF:(Svensson Eva Maria)
 

Search: WFRF:(Svensson Eva Maria) > New Dual Inhibitors...

New Dual Inhibitors of Bacterial Topoisomerases with Broad-Spectrum Antibacterial Activity and In Vivo Efficacy against Vancomycin-Intermediate Staphylococcus aureus

Durcik, Martina (author)
Univ Ljubljana, Fac Pharm, Ljubljana 1000, Slovenia.,University of Ljubljana, Slovenia
Cotman, Andrej Emanuel (author)
Univ Ljubljana, Fac Pharm, Ljubljana 1000, Slovenia.
Toplak, Zan (author)
Univ Ljubljana, Fac Pharm, Ljubljana 1000, Slovenia.
show more...
Mozina, Stefan (author)
Univ Ljubljana, Fac Pharm, Ljubljana 1000, Slovenia.;Lek Pharmaceut, Verovskova Ulica 57, Ljubljana 1000, Slovenia.
Skok, Ziga (author)
Lek Pharmaceut, Verovskova Ulica 57, Ljubljana 1000, Slovenia.
Szili, Petra Eva (author)
Biol Res Ctr, Synthet & Syst Biol Unit, Insti Biochem, H-6726 Szeged, Hungary.
Czikkely, Marton (author)
Biol Res Ctr, Synthet & Syst Biol Unit, Insti Biochem, H-6726 Szeged, Hungary.
Maharramov, Elvin (author)
Biol Res Ctr, Synthet & Syst Biol Unit, Insti Biochem, H-6726 Szeged, Hungary.,John Innes Ctr, Dept Biochem & Metab, Norwich NR4 7UH, Norfolk, Netherlands.
Vu, Thu Hien (author)
Biol Res Ctr, Synthet & Syst Biol Unit, Insti Biochem, H-6726 Szeged, Hungary.
Piras, Maria Vittoria (author)
Univ Ljubljana, Fac Pharm, Ljubljana 1000, Slovenia.;Univ Cagliari, Dipartimento Sci Chim & Geol, Monserrato, Ca, Italy.
Zidar, Nace (author)
Univ Ljubljana, Fac Pharm, Ljubljana 1000, Slovenia.
Ilas, Janez (author)
Univ Ljubljana, Fac Pharm, Ljubljana 1000, Slovenia.
Zega, Anamarija (author)
Univ Ljubljana, Fac Pharm, Ljubljana 1000, Slovenia.
Trontelj, Jurij (author)
Univ Ljubljana, Fac Pharm, Ljubljana 1000, Slovenia.
Pardo, Luis A. (author)
Max Planck Inst Multidisciplinar Sci, Oncophysiol, D-37075 Gottingen, Germany.
Hughes, Diarmaid, 1956- (author)
Uppsala universitet,Institutionen för medicinsk biokemi och mikrobiologi
Huseby, Douglas (author)
Uppsala universitet,Institutionen för medicinsk biokemi och mikrobiologi
Berruga-Fernández, Tália (author)
Uppsala universitet,Institutionen för medicinsk biokemi och mikrobiologi
Cao, Sha (author)
Uppsala universitet,Institutionen för medicinsk biokemi och mikrobiologi
Simoff, Ivailo (author)
Uppsala universitet,Institutionen för farmaci
Svensson, Richard (author)
Uppsala universitet,Institutionen för farmaci
Korol, Sergiy V. (author)
Uppsala universitet,Institutionen för medicinsk cellbiologi
Jin, Zhe (author)
Uppsala universitet,Institutionen för medicinsk cellbiologi
Vicente, Francisca (author)
Fdn Medina, Granada 18016, Spain.
Ramos, Maria C. (author)
Fdn Medina, Granada 18016, Spain.
Mundy, Julia E. A. (author)
John Innes Ctr, Dept Biochem & Metab, Norwich NR4 7UH, Norfolk, Netherlands.
Maxwell, Anthony (author)
John Innes Ctr, Dept Biochem & Metab, Norwich NR4 7UH, Norfolk, Netherlands.
Stevenson, Clare E. M. (author)
John Innes Ctr, Dept Biochem & Metab, Norwich NR4 7UH, Norfolk, Netherlands.
Lawson, David M. (author)
John Innes Ctr, Dept Biochem & Metab, Norwich NR4 7UH, Norfolk, Netherlands.
Glinghammar, Bjorn (author)
RISE,Kemisk och farmaceutisk toxikologi,RISE Res Inst Sweden, Dept Chem & Pharmaceut Toxicol, S-15136 Södertälje, Sweden.
Sjöström, Eva (author)
RISE,Kemiska processer och läkemedel
Bohlin, Martin (author)
RISE,Kemiska processer och läkemedel
Oreskär, Joanna (author)
RISE,Kemiska processer och läkemedel,RISE Res Inst Sweden, Dept Chem Proc & Pharmaceut Dev, S-15136 Södertälje, Sweden.
Alvér, Sofie (author)
RISE,Kemiska processer och läkemedel,RISE Res Inst Sweden, Dept Chem Proc & Pharmaceut Dev, S-15136 Södertälje, Sweden.
Janssen, Guido V. (author)
Sterk, Geert Jan (author)
Kikelj, Danijel (author)
Univ Ljubljana, Fac Pharm, Ljubljana 1000, Slovenia.
Pal, Csaba (author)
Biol Res Ctr, Synthet & Syst Biol Unit, Insti Biochem, H-6726 Szeged, Hungary.
Tomasic, Tihomir (author)
Univ Ljubljana, Fac Pharm, Ljubljana 1000, Slovenia.
Masic, Lucija Peterlin (author)
Univ Ljubljana, Fac Pharm, Ljubljana 1000, Slovenia.,University of Ljubljana, Slovenia
show less...
Univ Ljubljana, Fac Pharm, Ljubljana 1000, Slovenia University of Ljubljana, Slovenia (creator_code:org_t)
2023-03-06
2023
English.
In: Journal of Medicinal Chemistry. - : American Chemical Society (ACS). - 0022-2623 .- 1520-4804. ; 66:6, s. 3968-3994
Related links:
https://doi.org/10.1...
show more...
https://uu.diva-port... (primary) (Raw object)
https://urn.kb.se/re...
https://doi.org/10.1...
https://urn.kb.se/re...
show less...
  • Journal article (peer-reviewed)
Abstract Subject headings
Close  
  • A new series of dual low nanomolar benzothiazole inhibitors of bacterial DNA gyrase and topoisomerase IV were developed. The resulting compounds show excellent broad-spectrum antibacterial activities against Gram-positive Enterococcus faecalis, Enterococcus faecium and multidrug resistant (MDR) Staphylococcus aureus strains [best compound minimal inhibitory concentrations (MICs): range, <0.03125–0.25 μg/mL] and against the Gram-negatives Acinetobacter baumannii and Klebsiella pneumoniae (best compound MICs: range, 1–4 μg/mL). Lead compound 7a was identified with favorable solubility and plasma protein binding, good metabolic stability, selectivity for bacterial topoisomerases, and no toxicity issues. The crystal structure of 7a in complex with Pseudomonas aeruginosa GyrB24 revealed its binding mode at the ATP-binding site. Expanded profiling of 7a and 7h showed potent antibacterial activity against over 100 MDR and non-MDR strains of A. baumannii and several other Gram-positive and Gram-negative strains. Ultimately, in vivo efficacy of 7a in a mouse model of vancomycin-intermediate S. aureus thigh infection was also demonstrated.

Subject headings

MEDICIN OCH HÄLSOVETENSKAP  -- Medicinska och farmaceutiska grundvetenskaper -- Läkemedelskemi (hsv//swe)
MEDICAL AND HEALTH SCIENCES  -- Basic Medicine -- Medicinal Chemistry (hsv//eng)
MEDICIN OCH HÄLSOVETENSKAP  -- Medicinska och farmaceutiska grundvetenskaper -- Mikrobiologi inom det medicinska området (hsv//swe)
MEDICAL AND HEALTH SCIENCES  -- Basic Medicine -- Microbiology in the medical area (hsv//eng)
MEDICIN OCH HÄLSOVETENSKAP  -- Klinisk medicin -- Infektionsmedicin (hsv//swe)
MEDICAL AND HEALTH SCIENCES  -- Clinical Medicine -- Infectious Medicine (hsv//eng)

Keyword

antiinfective agent

Publication and Content Type

ref (subject category)
art (subject category)

Find in a library

To the university's database

Kungliga biblioteket hanterar dina personuppgifter i enlighet med EU:s dataskyddsförordning (2018), GDPR. Läs mer om hur det funkar här.
Så här hanterar KB dina uppgifter vid användning av denna tjänst.

 
pil uppåt Close

Copy and save the link in order to return to this view